Apparatus for curing a composite laminate

ABSTRACT

The present invention is related to a compound of formula (I): A-B-E-D (I), wherein: A is selected from the group consisting R a -L1-K-L2; and (II) B is either present or absent, but if B is present then B is (III), E is (IV), D is selected from the group comprising —(CR 1 R m ) r C(O)H, —(CR 1 R m ) r C—N, —CR 1 R m ) r NHNHC(O)NR 5 R 6 , —(CR 1 R m ) r C(O)(CR n R o ) r c(O)OR 7 , —(CR 1 R m ) r C(O)(Cr n R o ) r C(O)NR 8 R 9 , —(CR 1 R m ) r CH(OH)(Cr n R o ) r C(O)U, —(CR 1 R m ) r C(O)W—(CR 1 R m ) r C(O)CH 2 W, —(CR 1 R m ) r C(O)haloalkyl, and —(CR 1 R m ) r C(O)(CR n R o ) r —CHN 2 , and the use of said compounds as an inhibitor to rotamases.

The present invention is related to new compounds and the use of saidcompounds as an inhibitor to rotamases, for the manufacture ofmedicaments, for removing a rotamase from a sample, for identifying arotamase in a sample, for the manufacture of an affinity device, in drugpotentiation applications and methods of treating a patient.

Rotamases, also referred to as peptidyl-prolyl cis-trans isomerases(PPIases) are a class of enzymes important in protein folding, assemblyand transport. They act as catalysts to promote isomerization about thepeptidyl-prolyl bond, which can have profound effects on proteinfunction.

PPIases are divided into three families, cyclophilins, FK-506 bindingproteins (FXBPs) and the Pin1/parvulin family. While cyclophilins andFKBPs are distinguished by their ability to bind immununosuppressantmolecules cyclosporin and FK-506, respectively, the Pin1/parvulin familybinds neither of these immunosuppressants and is structurally unrelatedto the other two families. Known members of the Pin1/parvulin classinclude Pins 1-3 (Lu et al., Nature 380:544-547, 1996), Pin-L (Campbellet al., Genomics 44:157-162, 1997), parvulin (Rahfeld et al., FEBS Letts352:180-184, 1994), dodo (Maleszka et al., Proc Natl Acad Sci USA93:447-451, 1996) and Ess1/Pft1 (Hanes et al., Yeast 5:55-72, 1989; andHani et al., FEBS Letts 365:198-202, 1995).

Recent research suggests that members of the Pin1/parvulin family areessential modulators of the cell cycle, and mitosis in particular. Lu etal., Nature 380:544-547, 1996 reports that depletion of Pin1/Ess1 inyeast or human cells induces mitotic arrest followed by apoptosis,indicating that enzymes in this family serve an essential function incell division and proliferation.

Accordingly, compounds inhibiting rotamases can serve as agents for thetreatment of a variety of disorders which are characterized by aninappropriate cell proliferation including cancer and infectiousdiseases.

In the prior art a huge number of compounds are described which areactive as inhibitors to rotamase. The respective compounds are, amongothers, peptide derivatives such as amino methylene-peptides which aredescribed in European patent EP 0 610 743, or non-peptidic ornon-peptidomimetic molecules.

Given the importance of rotamase there is an ongoing need in the art toprovide further compounds which are suitable as inhibitors to rotamasesand thus suitable to be used as a medicament for those diseases whereina rotamase is involved in the pathological mechanism.

Accordingly, the problem underlying the present invention is to providecompounds which inhibit a rotamase. A further problem underlying thepresent invention is to provide new compounds for the treatment ofdiseases the pathophysiology of which involves an imbalanced orundesired activity of a rotamase. A still further problem underlying thepresent invention is to provide means for the isolation and/oridentification of rotamases.

In a first aspect the problem underlying the present invention is solvedby

a compound of formula (I):A-B-E-D  (I)wherein:A is selected from the group comprisingR^(a)-L1-K-L2-,

wherein the dashed lines indicate each and independently a single or adouble bond;wherein

-   -   K is selected from the group comprising        -   C=T,        -   O, S, S(O) and S(O₂),        -   or is absent,        -   with =T being selected from the group comprising            -   ═O, ═S, ═N—R¹, ═N—CN, ═N—NO₂ and ═CH—NO₂,    -   L1 and L2 are each and independently selected from the group        comprising        -   O, S and amines, preferably NR², NR³;        -   or being individually and independent from each other            absent;            B is either present or absent, but if B is present then B is            E is    -   whereby n is any integers from 1 to 5        -   whereby if n is 2 or more, any of the group(s)            —(CR^(j)R^(k))— which are present, can be the same as or            different from any other of the group(s) —(CR^(j)R^(k))—,            whereby any group —(CR^(j)R^(k))— is linked to any other            group —(CR^(j)R^(k))— or any moiety of the compound through            a bond, whereby the bond is selected from the group            comprising single bonds, double bonds and triple bonds;            D is selected from the group comprising            —(CR¹R^(m))_(r)C(O)H, —(CR¹R^(m))_(r)C≡N,            —(CR¹R^(m))_(r)NHNHC(O)NR₅R⁶,            —(CR¹R^(m))_(r)C(O)(CR^(n)R^(o))_(r′)C(O)OR⁷,            —(CR¹R^(m))_(r)C(O)(CR^(n)R^(o))_(r′)C(O)NR⁸R⁹,            —(CR^(j)R^(m))_(r)CH(OH)(CR^(n)R^(o))_(r′)C(O)U,            —(CR¹R^(m))_(r)C(O)W —(CR¹R^(m))_(r)C(O)CH₂W,            —(CR¹R^(m))_(r)C(O)haloalkyl, and            —(CR¹R^(m))_(r)C(O)(CR^(n)R^(o))_(r′)CHN₂,    -   whereby    -   U is —OR¹⁰ or —NR¹¹R¹², and    -   W is OR¹³, —SR¹⁴, —NR¹⁵R¹⁶, or a heterocyclic moiety,    -   whereby r and r′ are any integers from 0 to 5 and any r and r′        mentioned are independently selected from any other r and r′        mentioned or present,        -   whereby if r is 2 or more, any of the group(s) —(CR¹R^(m))—            which are present, can be the same as or different from any            of the other group(s) —(CR¹R^(m))—, whereby any group            —(CR¹R^(m))— is linked to any other group —(CR¹R^(m))— or            any moiety of the compound through a bond, whereby the bond            is selected from the group comprising single bonds, double            bonds and triple bonds, whereby if r′ is 2 or more, any of            the group(s) —(CR^(n)R^(o))— which are present, can be the            same as or different from any of the other group(s)            —(CR^(n)R^(o))—, whereby any group —(CR^(n)R^(o))— is linked            to any other group —(CR^(n)R^(o))— or any moiety of the            compound through a bond, whereby the bond is selected from            the group comprising single bonds, double bonds and triple            bonds;            Y is selected from the group comprising O, S, N—CN, N—NO₂,            CH—NO₂ or NR¹⁷, wherein R¹⁷ is selected from the group            comprising H, alkyl, substituted alkyl, cycloalkyl,            substituted cycloalkyl, alkylcycloalkyl, substituted            alkylcycloalkyl aryl, substituted aryl, alkylaryl,            substituted alkylaryl, heterocyclyl, substituted            heterocyclyl alkylheterocyclyl substituted alkylheterocyclyl            heteroaryl, substituted heteroaryl, alkylheteroaryl and            substituted alkylheteroaryl;            t is any integer from 1 to 6,    -   whereby if t is 2 or more, any of the group(s) —(CR^(d)R^(e))—        which are present, can be the same as or different from any of        the other group(s) —(CR^(d)R^(e))—, whereby any group        —(CR^(d)R^(e))— is linked to any other group —(CR^(d)R^(e))— or        any moiety of the compound through a bond, whereby the bond is        selected from the group comprising single bonds, double bonds        and triple bonds;        Z is        , whereby R_(X) is selected from the group comprising amino        acids, peptides, alkyl substituted alkyl, straight alkyl        substituted straight alkyl branched alkyl substituted branched        alkyl; or is absent; and Z is attached to any of the carbon of        the cyclic structure;        R^(a), R^(b), R^(c), R^(d), R^(e), R^(f), R^(g), R^(h), R^(i),        R^(j), R^(k), R^(l), R^(m), R^(n) and R^(o) are each and        independently from each other selected from the group comprising        H, OR¹⁸, SR¹⁹, NR²⁰R²¹, halo, alkyl substituted alkyl straight        alkyl, substituted straight alkyl, branched alkyl, substituted        branched alkyl, straight alkenyl, substituted straight alkenyl,        branched alkenyl, substituted branched alkenyl, straight        alkynyl, substituted straight alkynyl branched alkynyl,        substituted branched alkynyl cycloalkyl substituted cycloalkyl,        cycloalkenyl substituted cycloalkenyl, heterocyclyl, substituted        heterocyclyl mono-unsaturated heterocyclyl, poly-unsaturated        heterocyclyl mono-substituted poly-unsaturated heterocyclyl,        poly-substituted poly-unsaturated heterocyclyl, mono-substituted        mono-unsaturated heterocyclyl, poly-substituted mono-unsaturated        heterocyclyl, aryl, substituted aryl heteroaryl and substituted        heteroaryl; or may be independently from each other absent;        wherein, optionally, R^(d) and R^(f), R^(d) and R^(b), R^(d) and        R^(c) are linked so as to form a ring saturated or unsaturated        comprising 4 to 12 members, preferably 5 to 10 members;        wherein R¹, R², R³ and R⁴ are selected from the group comprising        H, alkyl substituted alkyl cycloalkyl substituted cycloalkyl,        alkylcycloalkyl, substituted alkylcycloalkyl, aryl substituted        aryl, alkylaryl, substituted alkylaryl heterocyclyl, substituted        heterocyclyl, alkylheterocyclyl, substituted alkylheterocyclyl,        heteroaryl substituted heteroaryl, alkylheteroaryl and        substituted alkylheteroaryl; and        R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁸, R¹⁹,        R²⁰ and R²¹ are each and independently selected from the group        comprising H, alkyl substituted alkyl aryl, substituted aryl,        alkylaryl, substituted alkylaryl, alkoxy, substituted alkoxy,        aryloxy, substituted aryloxy, alkylamino, substituted        alkylamino, arylamino and substituted arylamino;        or is a pharmaceutically acceptable salt, solvate, hydrate or        prodrug thereof.

As used herein in preferred embodiment

denotes any linkage to any other radical, moiety group or component of acompound, preferably of any compound as disclosed or described herein.

In an embodiment R^(b), R^(c), R^(d), R^(e), R^(f) and R^(g) are eachand independently from each other selected from the group comprising Hand alkyl preferably lower alkyl.

In an embodiment the dashed lines indicate a single bond.

In an embodiment K is selected from the group comprising

-   -   C=T    -   SO, S(O₂)    -   with =T being ═O or ═S.

In an embodiment L1 and L2 are each and independently selected from thegroup comprising NR² and NR³.

In a preferred embodiment R² and R³ are each and independently selectedfrom the group comprising H and alkyl, preferably lower alkyl.

In an embodimentA is selected from the group comprising

R²² is selected from the group comprising H, halogen, alkyl cycloalkyl,aryl, heterocyclyl, heteroaryl and derivatives of any of these groups;andR²³, R^(23′), R^(23″) are each independently selected from the groupconsisting of H, alkyl cycloalkyl aryl, heteroaryl and heterocyclyl andderivatives of any of these groups or is a pharmaceutically acceptablesalt or prodrug thereof.

In an embodiment Y is selected from the group comprising O, S and NR¹⁷,more preferably selected from the group comprising O and S.

In an embodiment, preferably an embodiment of the proceeding embodimentR⁴ is selected from the group comprising H and alkyl.

In a preferred embodiment the alkyl is a lower alkyl, preferably methyl.

In an embodiment n is 1 or 2.

In an embodiment, preferably an embodiment of the preceeding embodimentE is

R²⁴, R²⁵, R²⁶, and R²⁷ are each individually and independently selectedfrom the group comprising H, halogen, alkyl cycloalkyl, aryl,heterocyclyl, heteroaryl and derivatives of any of these groups.

In an embodiment, preferably any of the two preceeding embodiments, ifn=1, then r is different from 0.

In an alternative embodiment, if n=2, then r is any integer from 0 to 5,preferably 0, 1 or 2.

In an embodiment

D is selected from the group comprising —(CH₂)_(r)C(O)H, —(CH₂)_(r)C≡N,—(CH₂)_(r)NHNHC(O)NR⁵R⁶, —(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR⁷,—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR⁸R⁹, —(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U,—(CH₂)_(r)C(O)W —(CH₂)_(r)C(O)CH₂W, —(CH₂)_(r)C(O)haloalkyl, and—(CH₂)_(r)C(O)(CH₂)_(r′)CHN₂;

-   -   whereby    -   U is —R¹⁰ or —NR¹¹R¹²; and    -   W is 4R¹³, —SR¹⁴, —NR¹⁵R¹⁶, or a heterocyclic moiety,    -   whereby r and r′ is are any integers from 0 to 5 and any r and        r′ mentioned are independently selected from any other r and r′        mentioned or present and whereby any of R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰,        R¹¹, R¹², R¹³, R¹⁴, R¹⁵, and R¹⁶ are each and independently        selected from the group comprising H, alkyl, cycloalkyl, aryl,        heteroaryl and heterocyclyl and derivatives of any of these        groups.

In an embodiment D is —(CR¹R^(m))_(r)C≡N.

In an embodiment t is 2, 3 or 4.

In a second aspect of the present invention which is preferably anembodiment of the first aspect of the present invention the problemunderlying the present invention is solved by a compound having thestructure of formula (I)A-B-E-D  (I)wherein:A is selected from the group comprising

B is either present or absent, but if B is present, B is

E is

D is selected from the group comprising —(CH₂)_(r)C(O)H, —(CH₂)_(r′)C≡N,—(CH₂)_(r)NHNHC(O)NR_(A′)R_(A″), —C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR_(A′),—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR_(A′)R_(A″),—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W—CH₂)_(r)C(O)CH₂W,—(CH₂)_(r)C(O)haloalkyl, and —(CH₂)_(r)C(O)(CH₂)_(r′)CH₂;whereby

-   -   U is —OR_(A′) or —NR_(A′)R_(A″); and    -   W is —OR_(A′); —SR_(A′), —NR_(A′)R_(A″), or a heterocyclic        moiety,    -   whereby r and r′ are any integer from 0 to 5 and any r and r′        mentioned are independently selected from any other r and r′        mentioned or present; and whereby R_(A′) and R_(A″) are selected        independently from the group comprising H, alkyl, cycloalkyl        aryl, heteroaryl and heterocyclyl and derivatives of any of        these groups;        Y is O, S, or NR_(a) wherein R_(a) is selected from the group        comprising H, alkyl cycloalkyl, aryl, heteroaryl and        heterocyclyl and derivatives of any of these groups;        t is 1, 2 or 3;        Z is    -   , whereby R_(X) is selected from the group comprising amino        acids, peptides and alkyl;        R₁, R₃, R₄, R₆, R₇, R₈, and R₉ are each individually and        independently selected from the group comprising H, halogen,        alkyl, cycloalkyl, aryl, heterocyclyl, heteroaryl and        derivatives of any of these groups;        R₂, R₂′, R₂″, R₅ are each independently selected from the group        consisting of H, alkyl, cycloalkyl, aryl heteroaryl and        heterocyclyl and derivatives of any of these groups or is a        pharmaceutically acceptable salt or prodrug thereof, and        whereby        denotes any linkage to A, B, E and D, respectively.

In a preferred embodiment each of R₁, R₃, R₄, R₆, R₇, R₈ and R₉ isindividually and independently a derivative of any of alkyl, cycloalkyl,aryl heterocyclyl, or heteroaryl,

whereby any of these groups is individually and independentlysubstituted by one or more groups of the formula R_(b),

-   -   whereby R_(b) is selected from the group comprising alkyl,        cycloalkyl, aryl, heterocyclyl, heteroaryl, alkoxy, aryloxy,        arylalkoxy, alkoxycarbonyl, aryloxycarbonyl, alkanoyl, aroyl,        alkanoyloxy, aroyloxy, carbamoyl, carbamoyl derivative,        alkanoylamino, aroylamino, alkylthio, alkylthio derivatives,        arylthio, arylthio derivatives, ureido, ureido derivatives,        alkoxycarbonylamino, aryloxycarbonylamino, alkylcarbamoyloxy,        arylcarbamoyloxy, alkylsulfonylamino, arylsulfonylamino,        alkylaminosulfonyl, arylaminosulfonyl, amino, amino derivatives        and preferably R_(b) is further substituted by one or more        R_(c),    -   whereby R_(c) is selected from the group comprising alkyl        cycloalkyl, aryl, arylalkyl, alkoxy, aryloxy, arylalkoxy,        alkanoyl, aroyl, amino, halogen, hydroxy, oxo, carboxy, cyano,        nitro, amidino and guanidino.

In a further embodiment of the inventive compounds the carbamoyl groupis derivatized, preferably the nitrogen atom is independently mono- ordi-substituted by alkyl, aryl, heterocyclyl or heteroaryl; and/or

the alkylthio group is derivatized preferably the sulfur atom isoxidized to a sulfoxide or sulfone; and/or

the arylthio group is derivatized, preferably the sulfur atom isoxidized to a sulfoxide or sulfone; and/or

the ureido group is derivatized, preferably either the nitrogen atom isindependently mono- or di-substituted by a group which is selected fromthe group comprising alkyl aryl, heterocyclyl or heteroaryl,alkoxycarbonylamino, aryloxycarbonylamino, alklycarbamoyloxy,arylcarbamoyloxy, alkylsulfonylamino, arylsulfonylamino,alkylaminosulfonyl, arylaminosulfonyl; and/or

the amino group is derivatized, preferably the nitrogen atom isindependently mono- or di-substituted by alkyl aryl, heterocyclyl orheteroaryl, halogen, hydroxy, oxo, carboxy, cyano, nitro, amidino andguanidino.

In a particularly preferred embodiment B is present and has the meaningas defined in any of the preceding claims,E is

with R₆ to R₉ having the meaning as defined in any aspect or embodimentas specified herein.

In a more preferred embodiment D is selected from the group comprising—(CH₂)_(r)C(O)H, —(CH₂)_(r′)C≡N, —(CH₂)_(r)NHNHC(O)NR_(A′)R_(A″),—C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR_(A′),—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR_(A′)R_(A″),—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W,

whereby U is —OR_(A′) or —NR_(A′)R_(A″); W is —OR_(A′), —SR_(A′),—NR_(A′)R_(A″), or a heterocyclic moiety, r and r′ are independently anyinteger from 0 to 5; and R_(A′) and R_(A″) are selected independentlyfrom the group comprising H, alkyl, phenyl, benzyl, and phenethyl.

In an even more preferred embodiment D is —(CH₂)_(r)C≡N and r is anyinteger from 0 to 3.

In a further preferred embodimentB is

In a particularly preferred embodiment using the substituent B asdefined above, D is selected from the group comprising —(CH₂)_(r)C(O)H,—(CH₂)_(r′)C≡N, —(CH₂)_(r)NHNHC(O)NR_(A′)R_(A″),—C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR_(A′),—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR_(A′)R_(A″),—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W, whereby U is —OR_(A),or —NR_(A′)R_(A″), W is —OR_(A′), —SR_(A′), —NR_(A′)R_(A″), or aheterocyclic moiety; r and r′ are independently any integer from 0 to 5;and R_(A′) and R_(A″) are selected independently from the groupcomprising X alkyl, phenyl, benzyl, and phenethyl.

In an even more preferred embodiment D is —(CH₂)_(r)C≡N and r is anyinteger from 0 to 3.

In a further embodiment of the compounds according to the presentinventionA is

or a pharmaceutically acceptable salt or prodrug thereof.

In a preferred embodiment of the inventive compounds having Asubstituted as described above, D is selected from the group comprising—(CH₂)_(r)C(O)H, —(CH₂)_(r′)C≡N, —(CH₂)_(r)NHNHC(O)NR_(A′)R_(A″),—C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR_(A′),—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR_(A′)R_(A″),—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W; whereby U is —OR_(A′)or —NR_(A′)R_(A), W is —OR_(A′), —SR_(A′), —NR_(A′)R_(A″), or aheterocyclic moiety, R_(A), and R_(A″) are independently selected fromH, alkyl, phenyl, benzyl, and phenethyl; and r and r′ are independentlyany integer from 0 to 5. In an even more preferred embodiment D is—(CH₂)_(r)C≡N and r is any integer from 0 to 3.

In a further embodiment of the compounds according to the presentinvention B is absent and the other residues have the same meaning asdiscussed in any of the aforementioned aspects and embodiments,respectively, of the present invention.

In an even preferred embodiment with B being absent, D is selected fromthe group comprising —(CH₂)_(r)C(O)H, —(CH₂)_(r′)C≡N,—(CH₂)_(r)NHNHC(O)NR_(A′)R_(A″), —C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR_(A′),—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR_(A′)R_(A″),—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W;

whereby U is —OR_(A′) or —NR_(A′)R_(A″), W is —OR_(A), —SR_(A′),NR_(A′)R_(A″), or a heterocyclic moiety, R_(A′) and R_(A″) areindependently selected from H, alkyl, phenyl benzyl and phenethyl; and rand r′ are independently any integer from 0 to 5. In a more preferredembodiment D is —(CH₂)_(r)C≡N and r is any integer from 0 to 3.

Particularly preferred compounds according to the present invention arethe compounds specified in the following table:

-   3-(1H-Indol-3-yl)-2-acetylamino-propionic acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanomethylamide,-   3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-benzyl-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-o-tolyl-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(2-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-indan-5-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(2-phenyl-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-(1-Indol-3-yl)-2-(3-phenyl-4-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-phenoxy-phenyl-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Idol-3-yl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-cyclohexyl-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(2-fluoro-benzyl)-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-phenethyl-ureido)-ureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-ethyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-isopropyl-thioureido)propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-phenyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-methoxy-phenyl)-thioureido)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(thiophene-2-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-methoxy-benzenesulfonylamino)propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(quinoline-6-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-benzenesulfonylamino-propionic acid    cyanomethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,-   3-(1H-Indol-3-yl)-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl(1H-indol-3-yl)-butyramide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(H-indol-3-yl)-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(H-indol-3-yl)-ethyl]-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(H-indol-3-yl)-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)ethyl]-2-nitro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-1H-indol-3-yl)ethyl]-acrylamide,-   3-(1H-Indol-3-yl)-2,2-dimethyl-propionic acid cyanomethyl-amide,-   3-(1H-Indol-3-yl)-2-(2-methoxy-acetylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-1H-indol-3-yl)-ethyl]-oxalamic acid    methyl ester,-   N-[1-(Cyanomethyl-carbamoyl-2-(1H-indol-3-yl)-ethyl]-phthalamic    acid,-   N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-succinamic    acid,-   3-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl-carbamic acid    hexyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-1H-indol-3-yl)-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    9H-fluoren-9-ylmethyl ester,-   3-(1H-Indol-3-yl)-2-acetylamino-propionic acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)ureido]-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(1H-Idol-3-31)-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-benzyl-ureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Idol-3-yl)-2-(3-o-tolyl-ureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(1,1,3,3-tetramethyl-butyl)ureido]-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-indan-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Idol-3-yl)-2-[3-(1-phenyl-cyclopropyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-biphenyl-4-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-p-4-phenoxy-phenyl-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-cyclohexyl-ureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-ethyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-isopropyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-phenyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(thiophene-2-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-chloro-benzenesulfonylamino)propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(4-methoxy-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(quinoline-6-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-benzenesulfonylamino-propionic acid    cyanoethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-1H-indol-3-yl)-ethyl]-amide-   2-Propyl-pentanoic acid    [1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-1H-indol-3-yl)-ethyl]-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)ethyl]-amide,-   4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,-   3-(1H-indol-3-yl)-2-(2-1H-indol-3-yl-acetylamino)propionic acid    cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-4-(H-indol-3-yl)-butyramide,-   N-[1-Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-acrylamide,-   3-(1H-Indol-3-yl)-2,2-dimethyl-propionic acid cyanoethyl-amide,-   3-(1H-Indol-3-yl)-2-(2-methoxy-acetylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-oxalamic acid    methyl ester,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-phthalamic    acid,-   N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-succinamic    acid,-   3-[1-(Cyanoethyl-carbamoyl)-2-1H-indol-3-yl)ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    but-3-enyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    but-3-enyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid    9H-fluoren-9-ylmethylester,-   3-(4-Hydroxy-phenyl)-2-acetylamino-propionic acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethyl-phenyl)ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-benzyl-ureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-o-tolyl-ureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-indan-5-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-biphenyl-4-yl-ureido)propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-cyclohexyl-ureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-ethyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-isopropyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-phenyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-{3-[4-2,2,2-trifluoro-ethyl)phenyl]-thioureido}-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)    propionic acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-thiophene-2-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-trifluoromethoxy-benzenesulfonylamino)propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-chloro-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-methoxy-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(quinoline-6-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-benzenesulfonylamino-propionic acid    cyanomethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,-   3-(4-Hydroxy-phenyl)-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-1H-indol-3-yl-propionylamino)propionic    acid cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-4-(1H-indol-3-yl)-butyramide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-acrylamide,-   3-(4-Hydroxy-phenyl)-2,2-dimethyl-propionic acid cyanomethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(2-methoxy-acetylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-oxalamic    acid methyl ester,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-phthalamic    acid,-   N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-succinamic    acid,-   3-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)ethyl]-carbamic acid    methyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    9H-fluoren-9-ylmethyl ester,-   3-(4-Hydroxy-phenyl)-2-acetylamino-propionic acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-benzyl-ureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-o-tolyl-ureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(S)-(1-phenyl-ethyl)ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-indan-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-biphenyl-4-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(phenoxy-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-cyclohexyl-ureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-ethyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-isopropyl-thioureido)propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-phenyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(thiophene-2-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-chloro-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(4-methoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(quinoline-6-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-benzenesulfonylamino-propionic acid    cyanoethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,-   3-(4-hydroxy-phenyl)-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(3-1H-indol-3-yl-propionylamino)propionic    acid cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-4-(1H-indol-3-yl)-butyramide,-   N-[1-Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)ethyl]-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-fluoro-benzamide,-   N-[1-Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-acrylamide,-   3-(4-Hydroxy-phenyl)-2,2-dimethyl-propionic acid cyanoethyl-amide,-   3-(4-Hydroxy-phenyl)-2-(2-methoxy-acetylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-oxalamic    acid methyl ester,-   N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-phthalamic    acid,-   N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-succinamic    acid,-   3-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    but-3-enyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    but-3-enyl ester,-   [1-Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl)-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid    9H-fluoren-9-ylmethylester,-   3-Phenyl-2-acetylamino-propionic acid cyanomethyl-amide,-   3-Phenyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-benzyl-ureido)-propionic acid cyanomethyl-amide,-   3-Phenyl-2-(3-o-tolyl-ureido)propionic acid cyanomethyl-amide,-   3-Phenyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-indan-5-yl-ureido)-propionic acid cyanomethyl-amide,-   3-Phenyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-biphenyl-4-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-cyclohexyl-ureido)-propionic acid cyanomethyl-amide,-   3-Phenyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-3,4,5-trimethoxy-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-ethyl-thioureido)-propionic acid cyanomethyl-amide,-   3-Phenyl-2-(3-isopropyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-phenyl-thioureido)-propionic acid cyanomethyl-amide,-   3-Phenyl-2-[3-(4-fluoromethoxy-phenyl)-thioureido)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-{3-[(2,2,2-trifluoro-ethyl)-phenyl]-thioureido]-propionic    acid cyanomethyl-amide,-   3-Phenyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Phenyl-2-(thiophene-2-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(4-methoxy-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(quinoline-6-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-benzenesulfonylamino-propionic acid cyanomethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   3-Phenyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanomethyl-amide,-   3-Phenyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-4-(1H-indol-3-yl)-butyramide,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-acrylamide,-   3-Phenyl-2,2-dimethyl-propionic acid cyanomethyl-amide,-   3-Phenyl-2-(2-methoxy-acetylamino)-propionic acid cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-oxalamic acid methyl    ester,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-phthalamic acid,-   N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-succinamic acid,-   3-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethylcarbamoyl]-acrylic acid,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid isobutyl    ester,-   [1-Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid hexyl    ester,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid tert-butyl    ester,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid methyl    ester,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid ethyl    ester,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid    9H-fluoren-9-ylmethyl ester,-   3-Phenyl-2-acetylamino-propionic acid cyanoethyl-amide,-   3-Phenyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acid    cyanoethyl-amide-   3-Phenyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-(1 cyano-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-benzyl-ureido)propionic acid cyanoethyl-amide,-   3-Phenyl-2-(3-tolyl-ureido)-propionic acid cyanoethyl-amide,-   3-Phenyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-indan-5-yl-ureido)-propionic acid cyanoethyl-amide,-   3-Phenyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-biphenylyl-ureido)-propionic acid cyanoethyl-amide,-   3-Phenyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-(4-nitro-phenyl)-ureido)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-cyclohexyl-ureido)-propionic acid cyanoethyl-amide,-   3-Phenyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-ethyl-thioureido)-propionic acid cyanoethyl-amide,-   3-Phenyl-2-(3-isopropyl-thioureido)-propionic acid cyanoethyl-amide,-   3-Phenyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-phenyl-thioureido)-propionic acid cyanoethyl-amide,-   3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanoethyl-amide,-   3-Phenyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Phenyl-2-(thiophene-2-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(4-methoxy-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-quinoline-6-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-benzenesulfonylamino-propionic acid cyanoethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   3-Phenyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanoethyl-amide,-   3-Phenyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-4H-indol-3-yl)-butyramide,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-2-fluoro benzamide,-   N-[1-Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-acrylamide,-   3-Phenyl-2,2-dimethyl-propionic acid cyanoethyl-ramide,-   3-Phenyl-2-(2-methoxy-acetylamino)-propionic acid cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-oxalamic acid methyl    ester,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-phthalamic acid,-   N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-succinamic acid,-   3-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethylcarbamoyl]-acrylic acid,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid isobutyl    ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid butyl ester,-   [1-Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid cyanomethyl    ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid cyanomethyl    ester,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid but-3-enyl    ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid but-3-enyl    ester,-   [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid hexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid tert-butyl    ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid methyl    ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid ethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid    9H-fluoren-9-ylmethylester,-   3-Methylsulfanyl-2-acetylamino-propionic acid cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)ureido]-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-benzyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-o-tolyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(2,6-methyl-phenyl)ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-indan-S-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-biphenylyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-cyclohexyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-phenethyl-ureido)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-ethyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-isopropyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-phenyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-{3-[4-(2,2,2-trifluoro-ethyl)phenyl]-thioureido}-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-thiophene-2-sulfonylamino)propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Methylsulfanyl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(4-methoxy-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(quinoline-6-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-benzenesulfonylamino-propionic acid    cyanomethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   3-Methylsulfanyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanomethyl-amide,-   3-Methylsulfanyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl](1H-indol-3-yl)-butyramide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-acrylamide,-   3-Methylsulfanyl-2,2-dimethyl-propionic acid cyanomethyl-amide,-   3-Methylsulfanyl-2-(2-methoxy-acetylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl carbamoyl)-2-methylsulfanyl-ethyl]-oxalamic acid    methyl ester,-   N-[1-Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-phthalamic acid,-   N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-succinamic    acid,-   3-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfinyl-ethyl]-carbamic acid    isobutyl ester,-   [1-Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfinyl-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    9H-fluoren-9-ylmethyl ester,-   3-Methylsulfanyl-2-acetylamino-propionic acid cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethyl-phenyl)ureido]-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)ureido]-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-cyano-phenyl)ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-benzyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-o-tolyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(1,1,3,3-tetramethyl-butyl)ureido]-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-indan-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-biphenyl-4-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-cyclohexyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(2-fluoro-benzyl)ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-3,4,5-trimethoxy-phenyl)ureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-ethyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-isopropyl-thioureido)propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-nitro-phenyl)thioureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-phenyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-thiophene-2-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Methylsulfanyl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(4-methoxy-benzenesulfonylamino)propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(quinoline-6-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-benzenesulfonylamino-propionic acid    cyanoethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   3-Methylsulfanyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanoethyl-amide,-   3-Methylsulfanyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-4-(1H-indol-3-yl)-butyramide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-acrylamide,-   3-Methylsulfanyl-2,2-dimethyl-propionic acid cyanoethyl-amide,-   3-Methylsulfanyl-2-(2-methoxy-acetylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-oxalamic acid    methyl ester,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-phthalamic acid,-   N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-succinamic acid,-   3-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl-carbamic acid    but-3-enyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    but-3-enyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid    9H-fluoren-9-ylmethylester,-   3-Methanesulfonyl-2-acetylamino-propionic acid cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-benzyl-ureido)propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-o-tolyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(S)-(1-phenyl-ethyl)ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(2,6-dimethyl-phenyl)ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(1,1,3,3-tetramethyl-butyl)ureido]-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-indan-5-yl-ureido)propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(2-phenyl-cyclopropyl)ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-biphenyl-4-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-cyclohexyl-ureido)propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-ethyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-isopropyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-phenyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-(thiophene-2-sulfonylamino)propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Methanesulfonyl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(4-methoxy-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(quinoline-6-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-benzenesulfonylamino-propionic acid    cyanomethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   2-Propyl-pentanoic acid [1-(cyanomethyl-carbamoyl)-2-methanesulfonyl    ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   3-Methanesulfonyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanomethyl-amide,-   3-Methanesulfonyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-4-(1H-indol-3-yl-butyramide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-acrylamide,-   3-Methanesulfonyl-2,2-dimethyl-propionic acid cyanomethyl-amide,-   3-Methanesulfonyl-2-(2-methoxy-acetylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-oxalamic acid    methyl ester,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-phthalamic    acid,-   N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-succinamic    acid,-   3-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    9H-fluoren-9-ylmethyl ester,-   3-Methanesulfonyl-2-acetylamino-propionic acid cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethylsulfanyl-phenyl-ureido]-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-benzyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-o-tolyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(3-methyl-benzyl)ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(1,1,3,3-tetramethyl-butyl)ureido]-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-indan-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-biphenyl-4-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-cyclohexyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-methyl-benzyl)-ureido]-ionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-ethyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-isopropyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-phenyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-(thiophene-2-sulfonylamino)propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Methanesulfonyl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(4-methoxy-benzenesulfonylamino)propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-quinoline-6-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-benzenesulfonylamino-propionic acid    cyanoethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   3-Methanesulfonyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanoethyl-amide,-   3-Methanesulfonyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-4-(1H-indol-3-yl)-but    de,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-acrylamide,-   3-Methanesulfonyl-2,2-dimethyl-propionic acid cyanoethyl-amide,-   3-Methanesulfonyl-2-(2-methoxy-acetylamino)-propionic acid    cyanoethyl-amide,-   N-[1-Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-oxalamic acid    methyl ester,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-phthalamic    acid,-   N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-succinamic    acid,-   3-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]carbamic acid    but-3-enyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    but-3-enyl ester,-   [1-Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid    9H-fluoren-9-ylmethylester,-   3-Naphthalen-2-yl-2-acetylamino-propionic acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)ureido]-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-benzyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-o-tolyl-ureido)propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-indan-5-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(2-phenylcyclopropyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-biphenylyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-cyclohexyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-benzo[1,3]dioxol-S-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-ethyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-isopropyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(thiophene-2-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(4-methoxy-benzenesulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(quinoline-6-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-benzenesulfonylamino-propionic acid    cyanomethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   Thiophene-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   4-Acetylamino-N-[1-cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   3-Naphthalen-2-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(3-1H-indol-3-yl-propionylamino)propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-4-(1H-indol-3-yl)-butyramide,-   N-[1-Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-acrylamide,-   3-Naphthalen-2-yl-2,2-dimethyl-propionic acid cyanomethyl-amide,-   3-Naphthalen-2-yl-2-(2-methoxy-acetylamino)-propionic acid    cyanomethyl-amide,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-oxalamic acid    methyl ester,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic    acid,-   N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-succinamic    acid,-   3-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    hexyl ester,-   [1-Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    9H-fluoren-9-ylmethyl ester,-   3-Naphthalen-2-yl-2-acetylamino-propionic acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-benzyl-ureido)propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-o-tolyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-indan-S-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-biphenyl-4-yl-ureido)propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-phenoxy-phenyl)ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-nitrophenyl)ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-cyclohexyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-phenethyl-ureido)-ureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-ethyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-isopropyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)thioureido]-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino    propionic acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(thiophene-2-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(4-chloro-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(4-methoxy-benzenesulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-quinoline-6-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-benzenesulfonylamino-propionic acid    cyanoethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   2-Propyl-pentanoic acid    [1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   Thiophene-2-caboxylic acid [1    (cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   N-[1-Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,-   4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   3-Naphthalen-2-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic acid    cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(3-1H-indol-3-yl-propionylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-4-(1H-indol-3-yl)-butyramide,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   3-Chloromethyl-N-[1-cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   4-Chloromethyl-N-[1-cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-fluoro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-nitro-benzamide,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-acrylamide,-   3-Naphthalen-2-yl-2,2-dimethyl-propionic acid cyanoethyl-amide,-   3-Naphthalen-2-yl-2-(2-methoxy-acetylamino)-propionic acid    cyanoethyl-amide,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-oxalamic acid    methyl ester,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic    acid,-   N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-succinamic    acid,-   3-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethylcarbamoyl]-acrylic    acid,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    isobutyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    butyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    cyanomethyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    but-3-enyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    but-3-enyl ester,-   [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    2-isopropyl-5-methyl-cyclohexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    hexyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    tert-butyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    methyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    ethyl ester,-   [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid    9H-fluoren-9-ylmethylester,-   3-Benzo[b]thiophen-3-yl-2-acetylamino-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-benzyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-o-tolyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-indan-5-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-biphenylyl-ureido)propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-cyclohexyl-ureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-phenethyl-ureido)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-ethyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-isopropyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-phenyl-thioureido)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(thiophene-2-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-chloro-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-methoxy-benzenesulfonylamino)-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(quinoline-6-sulfonylamino)-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-benzenesulfonylamino-propionic acid    cyanomethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,-   2-Propyl-pentanoic acid    [2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [2-benzo[b]thiophen-3-yl-1-cyanomethyl-carbamoyl)-ethyl]-amide,-   Thiophene-2-carboxylic acid    [2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,-   4-Acetylamino-N-[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,-   3-Benzo[b]thiophen-3-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic    acid cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-1H-indol-3-yl-propionylamino)-propionic    acid cyanomethyl-amide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]4-(1H-indol-3-yl)-butyramide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-acrylamide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-acrylamide,-   3-Benzo[b]thiophen-3-yl-2,2-dimethyl-propionic acid    cyanomethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(2-methoxy-acetylamino)-propionic acid    cyanomethyl-amide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-oxalamic    acid methyl ester,-   N-[2-Benzo[b]thiophen-3-yl-1    cyanomethyl-carbamoyl)-ethyl]-phthalamic acid,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-succinamic    acid,-   3-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethylcarbamoyl]-acrylic    acid,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid isobutyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid butyl ester,-   [2-Benzo[b]thiophen-3-yl-1-cyanomethyl-carbamoyl)-ethyl]-carbamic    acid cyanomethyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid but-3-enyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid 2-isopropyl-5-methyl-cyclohexyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)ethyl]-carbamic    acid hexyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid tert-butyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid methyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid ethyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic    acid 9H-fluoren-9-ylmethyl ester,-   3-Benzo[b]thiophen-3-yl-2-acetylamino-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-benzyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-o-tolyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-2,6-dimethyl-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(1,1,3,3-ethyl-butyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-indan-5-yl-ureido)propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-adamantan-1-yl-ureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-biphenylyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-cyclohexyl-ureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-phenethyl-ureido)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-ethyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-isopropyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-thioureido)-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-phenyl-thioureido)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)    propionic acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(thiophene-2-sulfonylamino)-propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-chloro-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(4-methoxy-benzenesulfonylamino)-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(quinoline-6-sulfonylamino)propionic acid    cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-benzenesulfonylamino-propionic acid    cyanoethyl-amide,-   1-Methyl-1H-indole-2-carboxylic acid    [2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,-   2-Propyl-pentanoic acid    [2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,-   1-Methyl-cyclopropanecarboxylic acid    [2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,-   Thiophene-2-carboxylic acid    [2-benzo[b]thiophen-3-yl-1-cyanoethyl-carbamoyl)-ethyl]-amide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-3-trifluoromethyl-benzamide,-   Biphenyl-2-carboxylic acid    [2-benzo[b]thiophen-3-yl-1-cyanoethyl-carbamoyl)-ethyl]-amide,-   4-Acetylamino-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide,-   3-Benzo[b]thiophen-3-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic    acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(3-1H-indol-3-yl-propionylamino)-propionic    acid cyanoethyl-amide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-4-(1H-indol-3-yl)-butyramide,-   N-[2-Benzo[b]thiophen-3-yl-1 cyanoethyl-carbamoyl)-ethyl]-benzamide,-   3-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,-   4-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,-   N-[2-Benzo[b)thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-2-fluoro-benzamide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-2-nitro-benzamide,-   3-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide,-   3-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-2-fluoro-benzamide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-2-nitro-benzamide,-   3-Benzo[b]thiophen-3-yl-2,2-diethyl-propionic acid cyanoethyl-amide,-   3-Benzo[b]thiophen-3-yl-2-(2-methoxy-acetylamino)-propionic acid    cyanoethyl-amide,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-oxalamic    acid methyl ester,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-phthalamic    acid,-   N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)ethyl]-succinamic    acid,-   3-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethylcarbamoyl]-acrylic    acid,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid isobutyl ester,-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid carbamoylmethyl-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-2-methyl-propyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-2-hydroxy-ethyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-4-guanidino-butyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-2-phenyl-ethyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    [1-carbamoyl-2-(1H-indol-3-yl)ethyl]-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide-   3-[(1-Cyanomethyl-pyrrolidine-2-carbonyl)-amino]-succinamic acid-   D-1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-3-methyl-butyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-cyclohexyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    [1-carbamoyl-2-(4-trifluoromethyl-benzylsulfanyl)-ethyl]-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    [1-carbamoyl-2-(4-fluoro-benzylsulfanyl)-ethyl]-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    [1-carbamoyl-2-(4-fluoro-phenylmethanesulfonyl)-ethyl]-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (3-carbamoyl-phenyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    [1-carbamoyl-2-(1-methyl-1H-imidazol-4-yl)-ethyl]-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-2-pyridin-4-yl-ethyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-3-methyl-butyl)-amide-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid methyl ester-   1-Cyanomethyl-pyrrolidine-2-carboxylic acid-   N-(2-Cyanoethyl)-4-(4-dimethylamino-phenylazo)-benzenesulfonamide-   N-(2-Cyanoethyl)-trifluoromethoxy-benzenesulfonamide-   4-tert-Butyl-N-(2-cyanoethyl)-benzenesulfonamide-   4-Bromo-N-(2-cyanoethyl)-benzenesulfonamide-   4-Chloro-N-(2-cyanoethyl)-benzenesulfonamide-   N-(2-Cyanoethyl)₄-methoxy-benzenesulfonamide-   N-[4-(2-Cyanoethyl-sulfamoyl)-phenyl]-acetamide-   N-(2-Cyanoethyl)-4-methyl-benzenesulfonamide-   N-(2-Cyanoethyl)-benzenesulfonamide-   N-(2-Cyanoethyl)-C-phenyl-methanesulfonamide-   C,C,C-Trichloro-N-(2-cyanoethyl)-methanesulfonamide-   Butane-1-sulfonic acid (2-cyanoethyl)-amide-   Naphthalene-1-sulfonic acid (2-cyanoethyl)-amide-   Octane-1-sulfonic acid (2-cyanoethyl)-amide-   N-2-Cyanoethyl)-2,4,6-triisopropyl-benzenesulfonamide-   N-(2-Cyanoethyl)-2-trifluoromethyl-benzenesulfonamide-   N-[5-(2-Cyanoethyl-sulfamoyl)-4-methyl-thiazol-2-yl]-acetamide-   2-Bromo-N-(2-cyanoethyl)-benzenesulfonamide-   N-(2-Cyanoethyl)-2,4,6-trimethyl-benzenesulfonamide-   Thiophene-2-sulfonic acid (2-cyanoethyl)-amide-   N-(2-Cyanoethyl)-3-nitro-benzenesulfonamide-   1-(2-Cyanoethyl)-3-(4-nitro-phenyl)-thiourea-   1-(2-Cyano    1-(2-Cyano-ethyl)-3-phenyl-thioureaethyl)-3-phenyl-thiourea-   1-(2-Cyanoethyl)-3-(4-trifluoromethoxy-phenyl)-thiourea-   1-(2-Cyanoethyl)-3-(4-methylsulfanyl-phenyl)thiourea-   1-(2-Cyanoethyl)-3-(3,4,5-trimethoxy-phenyl)-thiourea-   1-(2-Cyanoethyl)-3-naphthalen-1-yl-thiourea-   1-Benzyl-3-(2-cyanoethyl)-thiourea-   1-Acetyl-3-(2-cyanoethyl)-thiourea-   1-(4-Azido-phenyl)-3-(2-cyanoethyl)-thiourea-   1-(2-Cyanoethyl)-3-(3-cyano-phenyl)-thiourea-   1-(2-Cyano1-(2-Cyano-ethyl)-3-(4-ethyl-phenyl)-thioureaethyl)-3-(4-ethyl-phenyl)-thiourea-   1-(2-Cyano1-(2-Cyano-ethyl-3-(4-cyano-phenyl)-thioureaethyl)-3-(4    cyano-phenyl)-thiourea-   1-Carbamoylmethyl-pyrrolidine-2-carboxylic acid    (1-carbamoyl-3-methyl-butyl)-amide1-(2-Cyanoethyl)-3-pyridin-4-yl-thiourea-   1-(2-Cyanoethyl)-3-(2,3,4-trifluoro-phenyl)-thiourea-   1-(2-Cyanoethyl)-3-(2,6-difluoro-phenyl)-thiourea-   1-(4-Bromo-phenyl)-3-(2-cyanoethyl)-thiourea-   1-(2-Cyanoethyl)-3-(4-methoxy-phenyl)-thiourea-   1-(2-Cyanoethyl)-3-m-tolyl-thiourea-   1-(2-Cyanoethyl)-3-p-tolyl-thiourea-   1-(2-Cyanoethyl)-3-cyclohexyl-urea-   1-(2-Cyanoethyl)-3-o-tolyl-urea-   1-(2-Cyanoethyl)-3-(2-methoxy-phenyl)-urea-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid butyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid cyanomethyl ester,-   [2-Benzo[b]thiophen-3-yl-1-cyanoethyl-carbamoyl)-ethyl]-carbamic    acid but-3-enyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid 2-isopropyl-5-methyl-cyclohexyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid hexyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid tert-butyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid methyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic    acid ethyl ester,-   [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)ethyl]-carbamic    acid 9H-fluoren-9-ylmethylester,    or a pharmaceutically acceptable salt, solvate, hydrate or prodrug    thereof.

Even more preferred compounds according to the present invention arethose mentioned in any of the tables herein and those further disclosedand/or characterized in the examples.

The problem underlying the present invention is also solved by thesubject matter of the independent claims. Preferred embodiments aredescribed in the dependent claims.

As used herein, each of the following terms, used alone or inconjunction with other terms, are defined as follows (except where notedto the contrary):

The term “alkyl” refers to a saturated aliphatic radical containing fromone to fourteen carbon atoms or a mono- or polyunsaturated aliphatichydrocarbon radical containing from two to twelve carbon atoms,containing at least one double and triple bound, respectively. “Alkyl”refers to both branched and unbranched alkyl groups. Preferred alkylgroups are straight chain alkyl groups containing from one to eightcarbon atoms. More preferred alkyl groups are straight chain alkylgroups containing from one to six carbon atoms and branched alkyl groupscontaining from three to six carbon atoms. It should be understood thatany combination term using an “alk” or “alkyl” prefix refers to analogsaccording to the above definition of “alkyl”. For example, terms such as“alkoxy”, “alkylthio” refer to alkyl group linked to a second group viaan oxygen or sulfur atom. “Alkanoyl” refers to an alkyl group linked toa carbonyl group (C═O). “Substituted alkyl” refers to alkyl groupsstraight or branched further bearing one or more substituents. Onesubstituent also means mono-substituted and more substitutents meanpoly-substituted. It should be understood that any combination termusing a “substituted alkyl” prefix refers to analogs according to theabove definition of “substituted alkyl”. For example, a term such as“substituted alkylaryl” refers to substituted alkyl group linked to anaryl group.

The term “lower alkyl” as used herein is preferably any alkyl asdisclosed herein, whereby the alkyl comprises one to six, preferably oneto five, and more preferably one or four C-atoms.

The term “cycloalkyl” refers to the cyclic analog of an alkyl group, asdefined above, optionally unsaturated and/or substituted. Preferredcycloalkyl groups are saturated cycloalkyl groups, more particularlythose containing from three to eight carbon atoms, and even morepreferably three to six carbon atoms. “Substituted cycloalkyl” refers tocycloalkyl groups further bearing one or more substituents.“Mono-unsaturated cycloalkyl” refers to cycloalkyl containing one doublebond or one triple bond. “Poly-unsaturated cycloalkyl” refers tocycloalkyl containing at least two double bonds or two triple bonds or acombination of at least one double bond and one triple bond.

The term “alkenyl” refers to an unsaturated hydrocarbon group containingat least one carbon-carbon double bond, including straight-chain,branched-chain, and cyclic groups. Preferred alkenyl groups have one totwelve carbons. More preferred alkenyl groups have one to six carbons.“Substituted alkenyl” refers to alkenyl groups further bearing one ormore substitutents.

The term “cycloalkenyl” refers to the cyclic analog of an alkenyl group,as defined above, optionally substituted. Preferred cycloalkenyl groupsare containing from four to eight carbon atoms. “Substitutedcycloalkenyl” refers to cycloalkenyl groups further bearing one or moresubstituents. “Mono-unsaturated cycloalkenyl” refers to cycloalkenylcontaining one double bond. “Poly-unsaturated cycloalkenyl” refers tocycloalkenyl containing at least two double bonds.

The term “alkynyl” refers to an unsaturated hydrocarbon group containingat least one carbon-carbon triple bond, including straight-chain,branched-chain, and cyclic groups. Preferred alynyl groups have one totwelve carbons. More preferred alkynyl groups have one to six carbons.“Substituted alkynyl” refers to alkynyl groups further bearing one ormore substitutents.

The term “aryl” refers to aromatic groups having in the range of 6 to 14carbon atoms and “substituted aryl” refers to aryl groups furtherbearing one or more substituents. It should be understood that anycombination term using an “ar” or “aryl” prefix refers to analogsaccording to the above definition of “aryl”. For example, a term such as“aryloxy” refers to aryl group linked to a second group via an oxygen.

Each of the above defined “alkyl”, “cycloalkyl”, and “aryl” shall beunderstood to include their halogenated analogs, whereby the halogenatedanalogs may comprise one or several halogen atoms. The halogenatedanalogs thus comprise any halogen radical as defined in the following.

The term “halo” refers to a halogen radical selected from the groupcomprising fluoro, chloro, bromo and iodo. Preferred halo groups arefluoro, chloro and bromo.

The term “heteroaryl” refers to a stable 5 to 8 membered, preferably 5or 6 membered monocyclic or 8 to 11 membered bicyclic aromaticheterocycle radical. Each heterocycle consists of carbon atoms and from1 to 4 heteroatoms selected from the group consisting of nitrogen,oxygen, and sulfur. The heterocycle may be attached by any atom of thecycle which results in the creation of a stable structure. Preferredheteroaryl radicals as used herein include, for example, furanyl,thienyl, pyrrolyl oxazolyl, thiazolyl, imidazolyl, pyrazolyl,isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, tetrazolyl,thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl,indolizinyl, indolyl, isoindolyl, benzofuranyl, benzothienyl, indazolyl,benzimidazolyl, benzthiazolyl, benzoxazolyl, purinyl, quinolizinyl,quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl,quinoxalinyl, naphthridinyl, pteridinyl carbazolyl, acridinyl,phenazinyl, phenothiazinyl and phenoxazinyl. “Substituted heteroaryl”refers to heteroaryl groups further bearing one or more substituents.

The term “heterocyclyl” refers to a stable 5 to 8 membered, preferably 5or 6 membered monocyclic or 8 to 11 membered bicyclic heterocycleradical which may be either saturated or unsaturated, and isnon-aromatic. Each heterocycle consists of carbon atom(s) and from 1 to4 heteroatoms selected from the group consisting of nitrogen, oxygen andsulfur. The heterocycle may be attached by any atom of the cycle, whichpreferably results in the creation of a stable structure. Preferredheterocycle radicals as used herein include, for example, pyrrolinyl,pyrrolidinyl, pyrazolinyl, pyrazolidinyl, piperidinyl, morpholinyl,thiomorpholinyl, pyranyl thiopyranyl, piperazinyl, indolinyl,azetidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrofuranyl,hexahydropyrimidinyl, hexahydropyridazinyl,1,4,5,6-tetrahydropyrimidin-2-ylamine, dihydro-oxazolyl,1,2-thiazinanyl-1,1-dioxide, 1,2,6-thiadiazinanyl-1,1-dioxide,isothiazolidinyl-1,1-dioxide and imidazolidinyl-2,4-dione.“Mono-unsaturated heterocyclyl” refers to heterocyclyl containing onedouble bond or one triple bond. “Poly-unsaturated heterocyclyl” refersto heterocyclyl containing at least two double bonds or two triple bondsor a combination of at least one double bond and one triple bond.

“Substituted heterocyclyl” refers to heterocyclyl groups further bearingone or more substituents.

The terms “heterocyclyl”, “heteroaryl” and “aryl”, when associated withanother moiety, unless otherwise specified, shall have the same meaningas given above. For example, “aroyl” refers to phenyl or naphthyl linkedto a carbonyl group (C═O).

Each aryl or heteroaryl unless otherwise specified includes itspartially or fully hydrogenated derivative. For example, quinolinyl mayinclude decahydroquinolinyl and tetrahydroquinolinyl, naphthyl mayinclude its hydrogenated derivatives such as tetrahydranaphthyl.

As used herein above and throughout this application, “nitrogen” or “N”and “sulfur” or “S” include any oxidized form of nitrogen such asnitrone, N-oxide and sulfur such as sulfoxide, sulfone and thequaternized form of any basic nitrogen such as HCl or TFA salts.

As used herein a wording defining the limits of a range of length suchas e.g. “1 to 5” means any integer from 1 to 5, i.e. 1, 2, 3, 4 and 5.In other words, any range defined by two integers explicitly mentionedis meant to comprise any integer defining said limits and any integercomprised in said range.

As used herein the term substituted shall mean that one or more H atomof the group or compound which is substituted, is replaced by adifferent atom, a group of atoms, a molecule or a molecule moiety. Suchatom, group of atoms, molecule or molecule moiety is also referred toherein as substituent.

The substituent can be selected from the group comprising hydroxy,alkoxy, mercapto, cycloalkyl, heterocyclic, aryl, heteroaryl, aryloxy,halogen, trifluoromethyl, difluoromethyl, cyano, nitrone, amino, amido,—C(O)H, acyl, oxyacyl carboxyl, carbamate, sulfonyl sulphonamide andsulfuryl. Any of the substituents may be substituted itself by any ofthe aforementioned substituents. This applies preferably to cycloalkylheterocylic, aryl heteroaryl and aryloxy. It is also preferred thatalkoxy and mercapto are those of a lower alkyl group. It is to beacknowledged that any of the definition provided herein also applies toany substituent. In preferred embodiments of the present invention asubstituent can also be selected from the group comprising K, L1, L2,R^(a) to R^(o) and R¹ to R²⁹, U, W, Y and Z.

As used herein =T can mean in any embodiment of the various aspects ofthe present invention that with =T is selected from electron withdrawinggroups, whereby preferably the electron withdrawing groups are selectedfrom ═O, ═N—R¹, —N—CN, ═N—NO₂ and ═CH—NO₂, and ═S,

It is within the present invention that any thiourea moieties andderivates therefrom, particularly those described herein, can, inprinciple be replaced by a cyanoguanidine moiety or residue andrespective derivates therefrom as described in J. Med. Chem 1977, 20,901-906. In Addition to being weakly basic cyanoguanidine and thioureaare also weakly acidic and both are therefore neutral and weaklyamphoteric compounds. Cyanoguanidine is also similar to thiourea in itsgeometry since both are planar structures with almost identical C—N bondlengths and bond angles. Another property common to thioureas andcyanoguanidines is conformational isomerism resulting from restrictedC—N bond rotation. Cyanoguanidine and thiourea are similar in theirhydrophilicity and hydrogen-bonding properties; they have comparably lowoctanol-water partition coefficients (P) and are both reasonably solublein water.

As used herein in connection with an embodiment of the various aspectsof the present invention the term “each and independently selected froma group” or “are independently from each other selected from the group”refers to two or more atoms, groups, substituents, moieties orwhatsoever and describes that the single atom, group etc. mentioned canbe selected from the group. The wording used is a truncation whichavoids unnecessary repetition as otherwise for each of the atoms, groupsetc. the same group definition would have to be repeated.

As used herein in connection with an embodiment of the various aspectsof the present invention the term “each and individually absent” refersto two or more atoms, groups, substituents, moieties or whatsoever anddescribes that the single atom, group etc. mentioned can be absentregardless whether any of the other atoms, groups etc. mentioned isabsent. The wording used is a truncation which avoids unnecessaryrepetition as otherwise for each of the atoms, groups etc. the fact thatit may be absent in an embodiment of the invention would have to berepeated.

In connection with the present invention some groups such as, e.g.,—(CR^(e)R^(d))— are repeated, i.e. are repeatedly present in a compoundaccording to the present invention. Typically such repetition occurs insuch a manner that, e.g., —(CR^(e)R^(d))— is repeated one or severaltimes. In case, e.g., —(CR^(e)R^(d))— is repeated one time which meansthat there are two consecutive groups of —(CR^(e)R^(d))—, these twoforms of —C(R^(e)R^(d)) can be either the same or they may be differentin a different embodiment which means that either R^(e) or R^(d) or bothof them are different between said two —(CR^(e)R^(d))— groups. If thereare three or more of these groups such as, e.g., —(CR^(e)R^(d))—, it ispossible that all of them are different or only some or differentwhereas others are the same in the sense defined above. Any permutationfor the arrangement for such identical or different groups is within thepresent invention.

It is to be acknowledged and within the present invention that anyradical, group, moiety or substituent as used herein can be linked orinserted in any orientation into any of the respective formulae orcompounds disclosed or described herein.

As used herein in connection with an embodiment of the various aspectsof the present invention the term referring to a group, substituent,moiety, spacer or the like specifying that it “can be inserted in anyorientation into any of the preceding formulae” means that the groupetc. can be attached to another atom, group, substitutent, moiety,spacer or the like of any of the compounds according to the presentinvention or any of the formulae disclosed herein via any of its endsand in particular through any of the atoms arranged at the ends of saidgroup, substituent, moiety, spacer or the like.

This applies particularly to asymmetric groups or radicals which canthus be, in principle, inserted in any orientation.

It is within the present invention that the features of the variousembodiments of the present invention can be realized either alone or incombination with the features of any other embodiment(s) of the presentinvention. Thus any combination of an/the individual feature or thecombination of features of an embodiment of the present invention withan/the individual feature(s) or the combination of features of any otherembodiment(s), either alone or in combination with other embodiments,shall be disclosed by the present specification.

It is to be understood that the term group as used herein in preferredembodiments, is also to mean or comprise radical and/or diradical or anyfurther radical having more than two free valences. It will beacknowledged by the ones skilled in the art that the various radicals orgroups are linked, preferably covalently linked, to another radical,group, component or moiety of the compound. Therefore, it is appropriateto understand that such groups are regarded as radicals. It will alsoacknowledged that a radical can, in principle, have either one, two,three or four free valences in case of a carbon atom, for binding to orwith other such radicals, groups, compounds or moieties. It is alsoacknowledged by the ones skilled in the art that the number of freevalences thus provided defines the number of radicals with which thefirst radical can form a covalent bonding.

Any of the compounds according to the present invention may be subjectto or result from a chemical transformation. Such transformationconverts the compound or the respective precursor thereof. The chemicaltransformation is selected from the group comprising hydrolysis,oxidation and reduction. Preferably, such chemical transformation is anenzymatic transformation. More preferably, the transformation is carriedout in vitro or in vivo. This kind of chemical transformation preferablyhappens to a prodrug which as such or the product thereof may bepharmaceutically active in the meaning of the present invention.

The compounds according to the present invention, the pharmaceuticalsalts thereof, products and any derivatives, may be modified such thatthe in vivo and/or in vitro enzymatic degradation, such as proteolyticdegradation, of said compounds is reduced or prevented. Generally, thisis done through the incorporation of synthetic amino acids, derivatives,or substituents into the respective compound. Preferably, only onenon-naturally occurring amino acid or amino acid side chain isincorporated into the compound, such that the targeting of the inhibitorof the appropriate enzyme is not significantly affected. However, someembodiments that use longer compounds according to the present inventioncontaining a number of targeting residues may tolerate more than onesynthetic derivative. In addition, non-naturally occurring amino acidsubstituents may be designed to mimic the binding of the naturallyoccurring side chain to the targeted enzyme, such that more than onesynthetic substituent is tolerated. Alternatively, peptide isosteres areused to reduce or prevent the compound's degradation. The resistance ofthe thus modified compound may be tested against the variety of knowncommercially available enzymes in vitro to determine the stabilityagainst enzymatic, preferably proteolytic, stability. Promisingcandidates may then be routinely screened in animal models, for exampleusing labeled compounds as described herein, to determine the in vivostability and efficacy.

In this embodiment, the resistance of the modified nonproteolyticreactive enzyme inhibitors may be tested against a variety of knowncommercially available nonproteolytic reactive enzymes in vitro todetermine their proteolytic stability. Promising candidates may then beroutinely screened in animal models, for example using labelledinhibitors, to determine the in vivo stability and efficacy.

In a still further aspect the compounds according to the presentinvention have at least one amino acid side chain. Preferably, the aminoacid side chain is in the (S) or L-configuration or in the (R) orD-configuration. Of said configurations the (S) or L-configuration isparticularly preferred.

In a preferred embodiment, the compound or pharmaceutically acceptablesalt or product of said compound according to the present inventioncomprises one or more non-naturally occurring amino acids or amino acidside chains. Alternatively or in addition thereto, said compounds maycomprise a peptide isostere.

In a further aspect the present invention is related to the use of acompound according to any of the aspects of the present invention as aninhibitor to or for a rotamase.

In an embodiment the rotamase regulates a part of the cell cycle.

In a preferred embodiment the rotamase regulates a part of the cellcycle, whereby preferably the part of the cell cycle is mitosis.

In an even more preferred embodiment the rotamase is a mammalianrotamase, preferably a human rotamase, more preferably hPin1.

In a further aspect the present invention is related to the use of thecompounds according to the present invention as a pharmaceutical or in apharmaceutical composition or for the manufacture of such pharmaceuticalcomposition which is preferably for the prophylaxis and/or treatment ofa disease, whereby preferably the disease involves a rotamase, wherebythe rotamase is a mammalian rotamase, preferably a human rotamase, morepreferably hPin1.

In connection with the further aspect of the present invention relatedto the use of any of the aforementioned compounds according to thepresent invention as an inhibitor to rotamases the following will beacknowledged by the one skilled in the art. In view of thecharacteristics of the compounds according to the present invention tobe active as an inhibitor of (a) rotamase(s), it is sufficient that therespective compound is at least suitable to inhibit at least onerotamase. The compounds according to the present invention which may beused as inhibitors, are also referred to as rotamase inhibitors herein.

Rotamases as such are known in the art and, for example, described inthe introductory part of this specification which is incorporated byreference. Rotamases as used herein shall preferably mean cyclophilins,FE-506 binding proteins and the rotamases of the Pin1/parvulin class.The Pin1/parvulin family includes Pins 1, PinL/parvulin, dodo, andEs1/Pft1. Suitable assays to determine whether a compound is suitable toinhibit a rotamase are known to the one skilled in the art and alsodescribed in the present examples. Basically, a rotamase is provided theactivity of which or non-activity of which may be determined. Acandidate inhibitor, i.e. a compound which is to be tested whether it isactive as an inhibitor to rotamase, is added to the rotamase and testedwhether upon the addition and/or influence of the candidate inhibitorthe activity of the rotamase is changed relative to the activity withoutcandidate rotamase inhibitor. If the rotamase activity is decreased bythe candidate rotamase inhibitor, said candidate rotamase inhibitor is arotamase inhibitor according to the present invention.

In another aspect of the present invention the compounds according tothe present invention may be used in a method for inhibiting a rotamase.In such case a rotamase is provided and a candidate rotamase inhibitoris added thereto whereupon the activity of rotamase is decreased.Optionally, such decrease in rotamase activity is measured. Thetechniques used theretofore are basically the same as outlined inconnection with the use of the compounds according to the presentinvention as rotamase inhibitors.

In another aspect of the present invention the compounds according tothe present invention are used in a method for quantifying the amount ofrotamase activity present in a sample and are for the same purposes usedin assays and diagnostic kits for the quantification of rotamases insamples such as blood, lymph, saliva or other tissue samples, bacterial,fungal, plant, yeast, viral or mammalian cell culture. Thus in apreferred embodiment, the sample is assayed using a standard substratefor the appropriate rotamase. A known concentration of a specificinhibitor according to the present invention is added, and allowed tobind to a particular rotamase present. The assay is then rerun, and theloss of activity is correlated to rotamase activity using techniqueswell known to those skilled in the art. Thus, methods of inhibiting arotamase are provided, wherein the rotamase inhibitors of the presentinvention may be added to a sample of rotamase or a sample where it isassumed that a rotamase activity is contained.

The compounds according to the present invention are preferablyreversible rotamase inhibitors.

By “reversible” herein is meant that the inhibitor binds non-covalentlyto the enzyme, and is to be distinguished from irreversible inhibition.See Walsh, Enzymatic Reaction Mechanisms, Freeman & Co., N.Y., 1979.“Reversible” in this context is a term understood by those skilled inthe art. Preferably the rotamase inhibitors according to the presentinvention are competitive inhibitors, that is, they compete withsubstrate in binding reversibly to the enzyme, with the binding ofinhibitor and substrate being mutually exclusive.

In a preferred embodiment of the compounds according to the presentinvention being active as a rotamase inhibitor, the dissociationconstant for inhibition of a rotamase with the inhibitor, generallyreferred to and characterized by those in the art as K_(i), is at mostabout 100 μM. By the term “binding constant” or “dissociation constant”or grammatical equivalents herein is meant the equilibrium dissociationconstant for the reversible association of inhibitor with enzyme. Thedissociation constants are defined and determined as described below.The determination of dissociation constants is known in the art. Forexample, for reversible inhibition reactions such as those of thepresent invention, the reaction scheme is as follows:

The enzyme (E) and the inhibitor (I) combine to give an enzyme-inhibitorcomplex (E*I). This step is assumed to be rapid and reversible, with nochemical changes taking place; the enzyme and the inhibitor are heldtogether by non-covalent forces. In this reaction, k₁ is the secondorder rate constant for the formation of the E*I reversible complex. k₂is the first order rate constant for the dissociation of the reversibleE*I complex. In this reaction, Ki=k₂/k₁.

The measurement of the equilibrium constant K_(i) proceeds according totechniques well known in the art. For example, assays generally usesynthetic chromogenic or fluorogenic substrates. The respective K_(i)values may be estimated using the Dixon plot as described by Irwin Segelin Enzyme Kinetics: Behavior and analysis of rapid equilibrium andsteady-state enzyme systems, 1975, Wiley-Interscience Publication, JohnWiley & Sons, New York, or for competitive binding inhibitors from thefollowing calculation:1−(ν_(i)/ν_(o))=[I]/[I]+K _(i)(1+([S]/K _(m))))  (Equation 2)wherein ν_(o) is the rate of substrate hydrolysis in the absence ofinhibitor, and ν_(i) is the rate in the presence of competitiveinhibitor.

It is to be understood that dissociation constants are a particularlyuseful way of quantifying the efficiency of an enzyme with a particularsubstrate or inhibitor, and are frequently used in the art as such. Ifan inhibitor exhibits a very low K_(i) value, it is an efficientinhibitor. Accordingly, the rotamase inhibitors of the present inventionhave dissociation constants, K_(i), of at most about 100 μM. Preferably,the rotamase inhibitors according to the present invention exhibitdissociation constants of at most about 10 μM, more preferably about 1μA most preferably of M, most about 100 nM.

The rotamase inhibitors of the present invention may be easily screenedfor their inhibitory effect. The inhibitor is first tested againstdifferent classes of rotamases for which the targeting group of theinhibitor was chosen, as outlined above. The activity of rotamases istypically measured by using a protease coupled assay with chromogenicsubstrates and conformer specific proteases. Basically, upon theconformer specific protease activity the chromogenic substrate isconverted into a compound which has an absorption characteristic whichis different from the starting chromogenic substrate and may thus beselectively measured. This reaction is accelerated in the presence ofthe rotamase and decelerated in the presence of rotamase-inhibitors.Alternatively, many rotamases and their corresponding chromogenicsubstrates are commercially available. Thus, a variety of rotamases areroutinely assayed with synthetic chromogenic substrates in the presenceand absence of the rotamase inhibitor, to confirm the inhibitory actionof the compound, using techniques well known in the art. The effectiveinhibitors are then subjected to kinetic analysis to calculate the K_(i)values, and the dissociation constants determined.

If a compound inhibits at least one rotamase, it is a rotamase inhibitorfor the purposes of the present invention. Preferred embodiments of therotamase inhibitors according to the present invention are compounds andinhibitors, respectively, that exhibit the correct kinetic parameters Kibelow 100 μM against the targeted rotamases.

In a further aspect of the present invention any of the compounds usedas rotamase inhibitors or as a medicament may be labelled.

By a “labelled rotamase inhibitor” herein is meant a rotamase inhibitorthat has at least one element, isotope or chemical compound attached toenable the detection of the rotamase inhibitor or the rotamase inhibitorbound to a rotamase. In general labels as used herein, fall into threeclasses: a) isotopic labels, which may be radioactive or heavy isotopes;b) immune labels, which may be antibodies or antigens; and c) colored orfluorescent dyes. The labels may be incorporated into the rotamaseinhibitor at any position. Examples of useful labels include ¹⁴C, ¹³C,¹⁵N, ³H, biotin, and fluorescent labels as are well known in the art.Examples for fluorescent labels are fluorescein, 6-FAM, HEX, TET, CY-5,CY-3, CY-7 and Texas Red.

In a further aspect the compounds according to the present invention,particularly those having rotamase inhibitory activity, may be used forremoving, identifying and/or inhibiting rotamases, preferablycontaminating rotamases, in a sample. Preferably, the sample is abiological sample. Even more preferably such sample is selected from thegroup comprising blood, lymph, saliva, tissue samples and bacterial,fungal, plant, viral and mammalian cell cultures.

In an embodiment of the present invention the rotamase inhibitors of thepresent invention are, for example, added to a sample where thecatalytic activity by contaminating rotamases is undesirable.Alternatively, the rotamase inhibitors of the present invention may bebound to a chromatographic support, using techniques well known in theart to form an affinity chromatography column. A sample containing anundesirable rotamase is run through the column to remove the rotamase.Alternatively, the same methods may be used to identity new rotamases.In doing so, a new rotamase contained in a sample may bind to therotamase inhibitor bound to the chromatographic support and uponelution, preferably a specific elution, from said chromatographicsupport, characterized and compared to other rotamase activities withregard to, among others, specificities. The characterization of therotamase as such is known to the one skilled in the art.

In a further aspect the present invention is related to a pharmaceuticalcomposition comprising a compound according to any of the aspects of thepresent invention and a pharmaceutically acceptable carrier, diluent orexcipient.

In an embodiment the composition comprises a further pharmaceuticallyactive compound, preferably such further pharmaceutically activecompound is a chemotherapeutic agent.

In a preferred embodiment of the composition the compound is present asa pharmaceutically acceptable salt or a pharmaceutically active solvate.

In an even more preferred embodiment the pharmaceutically activecompound is either alone or in combination with any of the ingredientsof the composition present in a multitude of individualized dosagesand/or administration forms.

In a further aspect the present invention is related to the use of thecompounds according to the present invention as a medicament and for themanufacture of a medicament, respectively.

This use of the compounds according to the present invention is based onthe fact that the compounds according to the present invention areinhibitors of rotamases and rotamases in turn have been identified inboth procaryotic and eucaryotic cells such as in bacteria, fungi, insectand mammalian cells. In this cellular environment rotamases are known tohave an impact on cell proliferation and mitosis, respectively. Becauseof this, rotamase inhibitors may be used for the treatment of a widevariety of disorders involving cell cycle regulation, both procaryoticand eucaryotic cell cycle regulation. The term “treatment” as usedherein comprises both treatment and prevention of a disease. It alsocomprises follow-up treatment of a disease. Follow-up treatment isrealized upon a treatment of a disease using compounds preferablydifferent from the one according to the present invention. For example,after stimulating the growth of a cell, tissue or the like by theapplication of a respective compound such as, e.g., erythropoietin, itmight be necessary to stop an overshooting reaction of cellproliferation which may be obtained using the compounds according to thepresent invention.

In a further aspect the present invention is related to the use of thecompounds according to the present invention as a medicament and for themanufacture of a medicament, respectively. It is to be understood thatany of the compounds according to the present invention can be used forthe treatment of or for the manufacture of a medicament for thetreatment of any of the diseases disclosed herein, irrespective of themode of action or the causative agent involved as may be specifiedherein. Of course, it may particularly be used for any form of suchdisease where the particular causative agent is involved. Causativeagent as used herein also means any agent which is observed inconnection with the particular disease described and such agent can bebut is not necessarily causative in the sense that is causes theobserved diseases or diseased condition.

In an embodiment the medicament is for the treatment or prevention of adisease, whereby the disease involves an undesired cell proliferation.

This use of the compounds according to the present invention is based onthe fact that the compounds according to the present invention aresuitable to inhibit undesired cell proliferation. Undesired cellproliferation comprises the undesired cell proliferation of procaryoticcells as well as undesired cell proliferation of eucaryotic cells. Theterm undesired cell proliferation also covers the phenomenon of abnormalcell proliferation, abnormal mitosis and undesired mitosis. Abnormalcell proliferation means any form of cell proliferation which occurs ina manner different from the normal cell proliferation. Normal cellproliferation is a cell proliferation observed under normalcircumstances by the majority of cells and organisms, respectively. Thesame basic definition applies to abnormal mitosis.

More particularly, undesired cell proliferation and undesired mitosismean a proliferation and a mitosis, respectively, which may be either anormal or an abnormal cell proliferation, however, in any case it is nota cell proliferation or mitosis which is desired. Desired may thus bedefined by an individual such as a human being and in particular aphysician, and defined within certain boundaries whereby the boundariesas such may reflect the extent of proliferation and mitosis,respectively, observed under usual conditions or in the majority ofcells and organisms, respectively, or may be arbitrarily fixed ordefined. Cell proliferation as used herein refers preferably to theproliferation of cells forming the organism to be treated or to which acompound according to the present invention shall be administered whichis also referred to herein as the first organism. Cell proliferation asused herein also means the proliferation of cells which are differentfrom the cells forming a first organism or species but are the cellsforming a second organism or second species. Typically, the secondorganism enters in or has a relationship with the first organism.Preferably, the first organism is a human being or an animal or plant,also referred to herein as patient, and the second organism is aparasite and pathogen, respectively, to said first organism. Mitosis asused herein, preferably means the cell division of cells being subjectto said cell proliferation whereby even more preferably mitosis is theprocess of cell division whereby a complete set of chromosomes isdistributed to the daughter cells.

Without wishing to be bound by any theory, it seems that the compoundsaccording to the present invention act on cells and thus influence theirproliferation and mitosis, respectively, by being inhibitors to someenzymatic activity. Preferably, the inhibition is reversible. Thisactivity is shown by the compounds according to the present inventionwith regard to bacteria, fungi, insect and mammalian cells.

Because of this, the compounds according to the present invention may beused for the treatment of a wide variety of disorders involving cellcycle regulation, both procaryotic and eucaryotic cell cycle regulation.The term “treatment” as used herein comprises both treatment andprevention of a disease. It also comprises follow-up treatment of adisease. Follow-up treatment is realized upon a treatment of a diseaseusing compounds preferably different from the one according to thepresent invention. For example, after stimulating the growth of a cell,tissue or the like by the application of a respective compound such as,e.g., erythropoietin, it might be necessary to stop an overshootingreaction of cell proliferation which may be obtained using the compoundsaccording to the present invention.

As used herein, the term “disease” describes any disease, diseasedcondition or pathological condition. Such disease may also be defined asabnormal condition. Also, in case of a pathogen, disease means acondition where a pathogen or an unwanted organism is present or presentin a concentration or compartment where it is undesired and thus subjectto reduction in numbers, removal, elimination and/or destruction byusing the compounds according to the present invention.

Cell proliferative disorders contemplated for treatment using thecompounds according to the present invention and for the methodsdisclosed herein include disorders characterized by unwanted orundesired, inappropriate or uncontrolled cell growth. Preferably, thedisease is selected from the group comprising neurodegenerativediseases, stroke, inflammatory diseases, immune based disorders,infectious diseases, heart diseases, fibrotic disorders, cardiovasculardiseases and cell proliferative diseases. Rotamases comprise families ofubiquitous and highly conserved enzymes who have been reported to playimportant roles in biological processes like protein folding,proteolysis, protein dephosphorylation, peptide transport function, cellcycle regulation, protein synthesis. Furthermore various isomerases havebeen shown to have regulatory functions as stable or dynamic part ofheterooligomeric complexes containing physiologically relevant proteinse.g. hormone receptors, ion channels, kinases, and growth factorreceptors.

Preferably, the neurodegenerative disease is selected from the groupcomprising Alzheimer's disease, Huntington's disease, Parkinson'sdisease, peripheral neuropathy, progressive supranuclear palsy,corticobasal degeneration, frontotemporal dementia, synucleinopathies,multiple system atrophy, amyotrophic lateral atrophy, prion diseases,and motor neuron diseases.

The compounds according to the present invention are additionally usefulin inhibiting cell cycle (mitosis) or cell division in pathogenicorganisms and are, therefore, useful for treating infectious diseases.

In a preferred embodiment the infectious is selected from the groupcomprising fungal, viral, bacterial and parasite infection.

Fungal infections contemplated for treatment using the compounds andmethods according to the present invention include systemic fungalinfections, dermatophytoses and fungal infections of the genito-urinarytract. Fungal infections, preferably systemic fungal infections, includethose caused by Histoplasma, Coccidioides, Cryptococcus, Blastomyces,Paracoccidioides, Aspergillus, Nocardia, Sporothrix, Rhizopus, Absidia,Mucor, Hormodendrum, Phialophora, Rhinosporidium, and the like.Dermatophyte infections include those caused by Microsporum,Trichophyton, Epidermophyton, Candida, Pityrosporum, and the like.Fungal disorders of the genito-urinary tract include infections causedby Candida, Cryptococcus, Aspergillus, Zygomycodoides, and the like.Infection by such organisms causes a wide variety of disorders such asringworm, thrush or candidiasis, San Joaquin fever or Valley fever orcoccidiodomycosis, Gilchrist's disease or blastomycosis, aspergillosis,cryptococcosis, histioplasmosis, paracoccidiomycosis, zygomycosis,mycotic keratitis, nail hair and skin disease, Lobo's disease,lobomycosis, chromoblastomycosis, mycetoma, and the like. Theseinfections can be particularly serious, and even fatal in patients witha depressed immune system such as organ transplant recipients andpersons with acquired immunodefficiency syndrome (AIDS). Insofar apatient group which can be treated using the inhibitors according to thepresent invention are persons with AIDS, particularly those sufferingfrom any of the aforementioned infectious diseases.

In a further embodiment the bacterial infection is selected from thegroup comprising infections caused by both Gram-positive andGram-negative bacteria, including infections caused by Staphylococcus,Clostridium, Streptococcus, Enterococcus, Diplococcus, Hemophilus,Neisseria, Erysipelothricosis, Listeria, Bacillus, Salmonella,Shzigella, Escherichia, Kiebsiella, Enterobacter, Serratia, Proteus,Morganella, Providencia, Yersinia, Camphylobacter, Mycobacteria,Helicobacter, Legionalla, Nocardia, and the like.

In a preferred embodiment the bacterial infection causes a wide varietyof diseases. Said disorders are selected, among others, from the groupcomprising pneumonia, diarrhea, dysentery, anthrax, rheumatic fever,toxic shock syndrome, mastoiditis, meningitis, gonorrhea, typhoid fever,brucellis, Lyme disease, gastroenteritis, tuberculosis, cholera, tetanusand bubonic plague.

In another embodiment the disease is a viral infection, moreparticularly a viral infection caused by a virus selected from the groupcomprising retrovirus, HIV, Papilloma virus, Polio virus, Epstein-Barr,Herpes virus, Hepatitis virus, Papova virus, Influenza virus, Rabies,JC, encephalitis causing virus, hemorrhagic fever causing virus (suchEbola Virus and Marburg Virus.

In a further embodiment the parasite infection is selected from thegroup comprising infections caused by Trypanosoma, Leishmania,Trichinella, Echinococcus, Nematodes, Classes Cestoda, Trenzatoda,Monogenea, Toxoplasma, Giardia, Balantidium, Paramecium, Plasmodium orEntamoeba.

The disease may further be a cell proliferative disorder whichpreferably is selected from the group characterized by unwanted,inappropriate or uncontrolled cell growth. Particular examples includecancer, fibrotic disorders, non-neoplastic growths. The neoplastic cellproliferative disorder is preferably selected from the group comprisingsolid tumors, and hematopoeitic cancers such as lymphoma and leukemia

More preferably, the solid tumor is selected from the group comprisingcarcinoma, sarcoma, osteoma, fibrosarcoma, and chondrosarcoma

More preferably, the cell proliferative disorder is selected from thegroup comprising breast cancer, prostate cancer, colon cancer, braincancer, lung cancer, pancreatic cancer, gastric cancer, bladder cancer,kidney cancer and head and neck cancer. Preferably, the lung cancer isnon-small lung cancer and small lung cancer.

In case the disease is a non-proliferative cell proliferative disorder,it is preferably selected from the group comprising fibrotic disorder.Preferably, the fibrotic disorder is fibrosis.

The disease may also be a non-neoplastic cell proliferative disorderwhich is selected from the group comprising prostatic hypertrophy,preferably benign prostatic hypertrophy, endometriosis, psoriasis,tissue repair and wound healing.

Fibrotic disorders which may be treated using the compounds according tothe present invention are generally characterized by inappropriateoverproliferation of non-cancerous fibroblasts. Examples thereof includefibromyalgia, fibrosis (cystic, hepatic, idopathic pulmonary,pericardial and the like), cardiac fibromas, fibromuscular hyperplasia,restenosis, atherosclerosis, fibromyositis, and the like.

In another embodiment the immune based and/or inflammatory disease is anautoimmune disease or autoimmune disorder. In a further embodiment, theimmune based and/or inflammatory disease is selected from the groupcomprising rheumatoid arthritis, glomerulonephritis, systemic lupuserythematosus associated glomerulonephritis, irritable bowel syndrome,bronchial asthma, multiple sclerosis, pemphigus, pemphigoid,scleroderma, myasthenia gravis, autoimmune haemolytic andthrombocytopenic states, Goodpasture's syndrome, pulmonary hemorrhage,vasculitis, Crohn's disease, and dermatomyositis.

In a further preferred embodiment the immune based and/or inflammatorydisease is an inflammatory condition.

In a still further embodiment the immune based and/or inflammatorydisease is selected from the group comprising inflammation associatedwith burns, lung injury, myocardial infarction, coronary thrombosis,vascular occlusion, post-surgical vascular reocclusion,artherosclerosis, traumatic central nervous system injury, ischemicheart disease and ischemia-reperfusion injury, acute respiratorydistress syndrome, systemic inflammatory response syndrome, multipleorgan dysfunction syndrome, tissue graft rejection and hyperacuterejection of transplanted organs.

In a further embodiment of the various aspects of the present inventionthe rotamase is human Pin1 and the rotamase involved in the mechanismunderlying the various diseases is human Pin1, respectively.

It is also within the present invention that the compounds according tothe present invention may be used for the treatment of a patientsuffering from a disease or disease condition as defined above. Suchtreatment comprises the administration of one or several of thecompounds according to the present invention or a medicament orpharmaceutical composition described herein.

Toxicity and therapeutic efficacy of a compound can be determined bystandard pharmaceutical procedures in cell culture or experimentalanimals. Cell culture assays and animal studies can be used to determinethe LD₅₀ (the dose lethal to 50% of a population) and the ED₅₀ (the dosetherapeutically effective in 50% of a population). The dose ratiobetween toxic and therapeutic effects is the therapeutic index, whichcan be expressed as the ratio LD₅₀/ED₅₀. Compounds which exhibit largetherapeutic indices are preferred. The data obtained from these cellculture assays and animal studies can be used in formulating a range ofdosages suitable for use in humans. The dosage may vary within thisrange depending upon a variety of factors, e.g., the dosage formemployed, the route of administration utilized, the condition of thesubject, and the like.

For any compound used according to the present invention, thetherapeutically effective dose can be estimated initially from cellculture assays by determining an IC₅₀ (i.e., the concentration of thetest substance which achieves a half-maximal inhibition of rotamaseactivity). A dose can then be formulated in animal models to achieve acirculating plasma concentration range that includes the IC₅₀ asdetermined in cell culture. Such information can be used to moreaccurately determine useful doses in humans. Levels in plasma may bemeasured, for example by HPLC.

It should be noted that the attending physician would know how to andwhen to terminate, interrupt, or adjust administration due to toxicity,to organ dysfunction, and the like. Conversely, the attending physicianwould also know to adjust treatment to higher levels if the clinicalresponse were not adequate (precluding toxicity). The magnitude of anadministered dose in the management of the disorder of interest willvary with the severity of the condition to be treated, with the route ofadministration, and the like. The severity of the condition may, forexample, be evaluated, in part, by standard prognostic evaluationmethods. Further, the dose and perhaps dose frequency will also varyaccording to the age, body weight, and response of the individualpatient. Typically, the dose will be between about 1-1000 mg/kg of bodyweight. About 1 mg to about 50 mg will preferably be administered to achild, and between 25 mg and about 1000 mg will preferably beadministered to an adult.

A program comparable to that discussed above may be used in veterinarymedicine. The exact dose will depend on the disorder to be treated andthe amount of rotamases to be inhibited, and will be ascertainable byone skilled in the art using known techniques. For example, as outlinedabove, some disorders are associated with increased levels of rotamases.

Depending on the specific conditions being treated, such agents may beformulated and administrated systemically or locally. Techniques forformulation and administration may be found in “Remington'sPharmaceutical Sciences”, 1990, 18^(th) ed., Mack Publishing Co.,Easton, Pa. The administration of a compound according to the presentinvention can be done in a variety of ways, including, but not limitedto, orally, subcutaneously, intravenously, intranasally, transdermally,intraperitoneally, intramuscularly, intrapulmonary, vaginally, rectally,or intraocularly, just to name a few. In some instances, for example, inthe treatment of wounds and inflammation, the rotamase inhibitors may bedirectly applied as a solution or spray.

In a further aspect the present invention is related to a medicament ora pharmaceutical composition comprising at least one active compound andat least one pharmaceutically acceptable carrier, excipient or diluent.As used herein, the active compound is a compound according to thepresent invention, a pharmaceutically salt or base thereof or a prodrugthereof, if not indicated to the contrary. The active compound may alsobe a pharmaceutically acceptable derivative of any of the compounds ofthe present invention. A pharmaceutically acceptable derivative refersto any pharmaceutially acceptable salt or ester of a compound of thepresent invention, however, is not limited thereto, or any othercompound which, upon administration to a patient, is capable ofproviding, either directly or indirectly, a compound of the presentinvention, a pharmacologically active metabolite or pharmacologicallyactive residue thereof.

For injection, compounds of the invention may be formulated in aqueoussolution, preferably in physiologically compatible buffers such asHank's solution, Ringer's solution, or physiologically saline buffer.For transmucosal administration, penetrants appropriate to the barrierto be permeated are used in the formulation. Such penetrants aregenerally known in the art.

The use of pharmaceutical acceptable carriers to formulate the compoundsaccording to the present invention into dosages or pharmaceuticalcompositions suitable for systemic administration is within the scope ofthe present invention. With proper choice of carrier and suitablemanufacturing practice, the compositions of the present invention, inparticular those formulated as solutions, may be administeredparenterally, such as by intravenous injection. The compounds can bereadily formulated using pharmaceutically acceptable carriers well knownin the art into dosages suitable for oral administration. Such carriersenable the compounds according to the present invention to be formulatedas tablets, pills, capsules, dragees, liquids, gels, syrups, slurries,suspensions and the like, for oral ingestion by a subject to be treated.Suitable pharmaceutical carriers include, but are not limited to, water,salt solutions, alcohols, polyethylene glycols, gelatine, carbohydrates,such as lactose, amylose or starch, magnesium stearate, talc, silicicacid, viscous paraffine, fatty acid esters, hydroxymethylcellulose,polyvinylpyrolidone and the like.

Compounds according to the present invention or medicaments comprisingthem intended to be administered intracellularly may be administeredusing techniques well known to those of ordinary skill in the art. Forexample, such agents may be encapsulated into liposomes, thenadministered as described above. Liposomes are spherical lipid bilayerswith aqueous interiors. All molecules present in an aqueous solution atthe time of liposome formation are incorporated into the aqueousinterior. The liposomal contents are both protected from the externalmicroenvironment and, because liposomes fuse with cell membranes, areefficiently delivered into the cell cytoplasm. Delivery systemsinvolving liposomes are discussed in International Patent PublicationNo. WO 91/19501, as well as U.S. Pat. No. 4,880,635 to Janoff et al. Thepublications and patents provide useful descriptions of techniques forliposome drug delivery and are incorporated by reference herein in theirentirety.

Pharmaceutical compositions comprising a compound according to thepresent invention for parenteral administration include aqueoussolutions of the active compound(s) in water-soluble form. Additionally,suspensions of the active compounds may be prepared as appropriate oilyinjection suspensions. Suitable lipophilic solvents or vehicles includefatty oils such as sesame oil, or synthetic fatty acid esters, such asethyl oleate or triglycerides, or liposomes. Aqueous injectionssuspensions may contain compounds which increase the viscosity of thesuspension, such as sodium carboxymethyl cellulose, sorbitol, dextran,or the like. Optionally, the suspension may also contain suitablestabilizers or agents which increase the solubility of the compounds toallow for the preparation of highly concentrated solutions.

Pharmaceutical compositions comprising a compound according to thepresent invention for oral use can be obtained by combining the activecompound(s) with solid excipient, optionally grinding the resultingmixture, and processing the mixture of granules, after adding suitableauxiliaries, if desired, to obtain tablets or dragee cores.

Suitable excipients are, in particular, fillers such as sugars,including lactose, sucrose, mannitol, sorbitol, and the like; cellulosepreparations, such as, for example, maize starch, wheat starch, ricestarch, potato starch, gelatin, gum tragacanth, methyl cellulose,hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose,polyvinylpyrrolidone (PVP) and the like, as well as mixtures of any twoor more thereof. If desired, disintegrating agents may be added, such ascross-linked polyvinyl pyrrolidone, agar, alginic acid or a salt thereofsuch as sodium alginate, and the like.

Dragee cores as a pharmaceutical composition comprising a compoundaccording to the present invention are provided with suitable coatings.For this purpose, concentrated sugar solutions may be used, which mayoptionally contain gum arabic, talc, polyvinyl pyrrolidone, carbopolgel, polyethylene glycol, titanium dioxide, lacquer solutions, suitableorganic solvents or solvent mixtures, and the like. Dyestuffs orpigments may be added to the tablets or dragee coatings foridentification or to characterize different combinations of activecompound doses.

Pharmaceutical preparations comprising a compound according to thepresent invention which can be used orally include push-fit capsulesmade of gelatin, as well as soft, sealed capsules made of gelatin and aplasticizer, such as glycerol or sorbitol. The push-fit capsules cancontain the active ingredients in admixture with filler such as lactose,binders such as starches and/or lubricants such as talc or magnesiumstearate and, optionally, stabilizers. In soft capsules, the activecompounds may be dissolved or suspended in suitable liquids, such asfatty oils, liquid paraffin, or liquid polyethylene glycols. Inaddition, stabilizers may be added.

A “patient” for the purposes of the present invention, i.e. to whom acompound according to the present invention or a pharmaceuticalcomposition according to the present invention is administered, includesboth humans and other animals and organisms. Thus the compounds,pharmaceutical compositions and methods are applicable to or inconnection with both human therapy and veterinary applications. Forexample, the veterinary applications include, but are not limited to,canine, bovine, feline, porcine, caprine, equine, and ovine animals, aswell as other domesticated animals including reptiles, such as iguanas,turtles and snakes, birds such as finches and members of the parrotfamily, lagomorphs such as rabbits, rodents such as rats, mice, guineapigs and hamsters, amphibians, fish, and arthropods. Valuablenon-domesticated animals, such as zoo animals, may also be treated. Inthe preferred embodiment the patient is a mammal, and in the mostpreferred embodiment the patient is human.

The pharmaceutical composition according to the present inventioncomprises at least one compound according to the present invention,preferably a rotamase inhibitor according to the present application, ina form suitable for administration to a patient. Preferably, a compoundaccording to the present application is in a water soluble form, such asbeing present as a pharmaceutically acceptable salt, which is meant toinclude both acid and base addition salts. “Pharmaceutically acceptableacid addition salt” refers to those salts that retain the biologicaleffectiveness of the free bases and that are not biologically orotherwise undesirable, formed with inorganic acids such as hydrochloricacid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid andthe like, and organic acids such as acetic acid, propionic acid,glycolic acid, pyruvic acid, oxalic acid, maleic acid, malonic acid,succinic acid, fumaric acid, tartaric acid, citric acid, benzoic acid,cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid,p-toluenesulfonic acid, salicylic acid and the like. “Pharmaceuticallyacceptable base addition salts” include those derived from inorganicbases such as sodium, potassium, lithium, ammonium, calcium, magnesium,iron, zinc, copper, manganese, aluminum salts and the like. Particularlypreferred are the ammonium, potassium, sodium, calcium, and magnesiumsalts. Salts derived from pharmaceutically acceptable organic non-toxicbases include salts of primary, secondary, and tertiary amines,substituted amines including naturally occurring substituted amines,cyclic amines and basic ion exchange resins, such as isopropylamine,trimethylamine, diethylamine, triethylamine, tripropylamine, andethanolamine. The pharmaceutical compositions according to the presentinvention may also include one or more of the following: carrierproteins such as serum albumin; buffers; fillers such asmicrocrystalline cellulose, lactose, corn and other starches; bindingagents; sweeteners and other flavoring agents; coloring agents; andpolyethylene glycol. Additives are well known in the art, and are usedin a variety of formulations.

The compounds according to the present invention are, in a furtherembodiment, administered to a subject either alone or in apharmaceutical composition where the compound(s) is mixed with suitablecarriers or excipient(s). In treating a subject, a therapeuticallyeffective dose of compound (i.e. active ingredient) is administered. Atherapeutically effective dose refers to that amount of the activeingredient that produces amelioration of symptoms or a prolongation ofsurvival of a subject which can be determined by the one skilled in theart doing routine testing.

On the other hand, the compounds according to the present inventionwhich have a rotamase inhibitory activity may as such or contained in apharmaceutical composition according to the present invention be used indrug potentiation applications.

For example, therapeutic agents such as antibiotics or antitumor drugscan be inactivated through the catalytic action of endogenous rotamases,thus rendering the administered drug less effective or inactive.Accordingly, the rotamase inhibitors of the invention may beadministered to a patient in conjunction with a therapeutic agent inorder to potentiate or increase the activity of the drug. Thisco-administration may be by simultaneous administration, such as amixture of the rotamase inhibitor and the drug, or by separatesimultaneous or sequential administration.

According to the present invention the compounds disclosed herein,referred to as compounds according to the present invention, may be usedas a medicament or for the manufacture of medicament or in a method oftreatment of a patient in need thereof. Insofar any of these compoundsconstitute a pharmaceutical compound. The use of this kind of compoundalso comprises the use of pharmaceutically acceptable derivatives ofsuch compounds.

In addition, the compounds according to the present invention may betransformed upon application to an organism such as a patient, into thepharmaceutically active compound. Insofar the compounds according to thepresent invention may be prodrugs which, however, are nevertheless usedfor the manufacture of the medicaments as disclosed herein given thefact that at least in the organism they are changed in a form whichallows the desired pharmaceutical effect.

It is to be understood that any of the pharmaceutical compositionsaccording to the present invention may be used for any of the diseasesor conditions described herein.

The pharmaceutical compositions according to the present invention maybe manufactured in a manner that itself is known, e.g., by means ofconventional mixing, dissolving, granulating, dragee-mixing, levigating,emulsifying, encapsulating, entrapping, lyophilizing, processes, or thelike.

In a further aspect of the present invention the compounds of thepresent invention may be used as insecticides as they may prevent cellcycle mitosis in insect cells and thus can be used to control the growthand proliferation of a variety of insect pests. This aspect of thepresent invention has important applications in agriculture, such as inthe field, in the storage of agricultural products and the like.Additionally, the compounds according to the present invention areuseful for controlling insect populations, preferably in placesinhabited by men, such as homes, offices and the like.

Any of the compounds according to the present invention containing oneor more asymmetric carbon atoms may occur as racemates and racemicmixtures, single enantiomers, diastereomeric mixtures and individualdiastereomers. All such isomeric forms of these compounds are expresslyincluded in the present invention. Each stereogenic carbon may be in theR or S configuration, or a combination of configurations.

It shall be understood by one of ordinary skill in the art that allcompounds of the invention are those which are chemically stable. Thisapplies to any of the various uses of the compounds according to thepresent invention disclosed herein.

In determining the suitability of any of the compounds according to thepresent applications for the various uses, besides the particularprofile to be met by such a compound, also it has to be checked whetherit is stable to proteolytic degradation. The resistance of the compoundused as rotamase inhibitor or pharmaceutical may be tested against avariety of non-commercially available rotamases in vitro to determineits proteolytic stability. Promising candidates may then be routinelyscreened in animal models, for example using labelled inhibitors, todetermine the in vivo stability and efficacy. In any of theaforementioned uses the compound may be present in a crude or purifiedform. Methods for purifying the compounds according to the presentinvention are known to the one skilled in the art.

The invention is now further illustrated by reference to the followingfigure and examples from which further advantages, features andembodiments may be taken. It is understood that these examples are givenfor purpose of illustration only and not for purpose of limitation. Allreferences cited herein are incorporated by reference.

FIGS. 1 to 6 b show various methods for the synthesis of the compoundsaccording to the present invention which will be explained in moredetail in the following examples.

EXAMPLE 1 General Synthetic Methods

Compounds of the invention may in principle be synthesized by methodsdescribed below. In addition, further methods for the synthesis of theknown compounds used according to the present invention are described,for example, in WO 01/19816, WO 01/30772, US patent application2001/0046207, U.S. Pat. No. 4,927,809; WO 00/55126, WO 99/56765, WO01/09110, WO 01/47886, WO 00/49008, WO 99/24460, WO 00/51998, WO00/48992 and WO 01/49288. Standard peptide coupling, protection anddeprotection reactions (M. Bodansky, The Practice of Peptide Synthesis,Springer-Verlag, 1984) are employed in these syntheses.

As used herein, the following abbreviations are used.

Ar is argon;

Boc is tertiary butoxy carbamoyl;

Bth is benzo[b]thiophen-2-yl;

t-Bu is tertiary butyl;

DCM is dichloromethane;

DIC is diisopropyl carbodiimide;

DIPEA is N,N-diisopropylethylanmine;

DMF is N,N-dimethylformamide;

DMSO is N,N-dimethylsulfoxide;

eq is equivalent;

Et₃N is triethylamine;

EtOAc is ethyl acetate;

HBTU is 2-(1H-benzotriazole-1-yl)-1, 1,3,3-tetramethyluroniumhexafluorophosphate;

HPLC is high performance liquid chromatography;

h is hour;

MeOH is methanol;

MgSO₄ is magnesium sulfate;

NaCl is sodium chloride;

NaHCO₃ is sodium hydrogencarbonate;

NaL is naphthalene-2-yl;

PyBrOP is benzotriazole-1-yl-oxy-tris-pyrrolidino-phosphoniumhexafluorophosphate;

TFA is trifluoroacetic acid

According to scheme 1 depicted in FIG. 1 suitable protected amino acidderivatives 1 bearing R₅, R₆, R₇ and 4 bearing R₅, R₆, R₇, R₈, R⁹ aretransformed to the corresponding primary amides 2 and 5 using ammonia orammonium chloride under standard coupling conditions typically used inpeptide synthesis. Suitable protecting groups (R₅) for the aminofunctions are the t-butoxycarbonyl (Boc), 9-fluorenylmethoxycarbonyl(Fmoc), and other groups. Examples of standard coupling conditions wouldbe reacting the protected amino acid derivatives 1 and 4 in the presenceof a coupling reagent such asbenzotriazol-1-yloxytrispyrrolidinophosphonium hexafluorophosphate(PyBOP®), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride(EDCl), O-benzotriazol-1-yl-N,N,N′,N′-tetramethyluroniumhexafluorophosphate (HBTU), 1,3-dicyclohexylcarbodiimide (DCC), or thelike, in a suitable solvent (N-methylpyrrolidinone, DMF, DCM, or thelike). Additionally an appropriate catalyst (e.g.,1-hydroxybenzotriazole (HOBT), 1-hydroxy-7-azabenzotriazole (HOAt), orthe like) and non-nucleophilic bases (e.g., N-methylmorpholine,triethylamine, N,N-diisopropylethylamine or the like, or any suitablecombination thereof) may be added. The resulting amides are converted tothe corresponding nitriles 3 and 6 by dehydration. Suitabledehydratation conditions can be cyanuric chloride in DMF,trifluoroacetic anhydride in DCM in the presence of pyridine (N. D.Hone, L. J: Payne, C. M. Tice, Tetrahedron Lett., (2001) 42, 1115-1118),benzoylsulfonyl chloride in pyridine (T. T. Van, E. Kojro, Z. Grzonka,Tetrahedron (1977) 33, 2299).

According to scheme 2 depicted in FIG. 2 suitable protected buildingblock derivatives 8 bearing R₅, R₆, R₇ and 10 bearing R₅, R₆, R₇, R₈, R₉are reacted with activated amino acid derivatives 7 bearing R₂, R₃, R₄under standard coupling conditions used in peptide synthesis theresulting derivatives 9 and 11 are obtained after deprotection of theamine.

According to scheme 3a depicted in FIG. 3 a a suitable protected amines9 bearing R₂, R₃, R₄, R₅, R₆, R₇ are allowed to react with differentreagents. They can be reacted with acids, acyl chlorides or anhydridesto provide 9a. Acids can be condensed by standard peptide couplingconditions such as PyBrOP, DIPEA,1-hydroxybenzotriazole-6-sulfonamidomethyl polystyrene in dry DMF (I. E.Pop, J. Org. Chem. (1997) 62, 2594). Acyl chlorides or anhydrides can bereacted in dry DCM in the presence of a non nucleophilic base like DIPEAfollowed by sequestering any remaining acyl chlorides or anhydride by apolymer-supported quenching reagent like tris-2-aminoethyl)-aminepolystyrene (R. J. Booth, J. C. Hodges, J. Am. Chem. Soc. (1997) 119,4882; M. W. Creswell, G. L. Bolton, J. C. Hodges, M. Meppen, Tetrahedron(1998) 54, 3983). Sulfonamide derivatives 9b are obtained after reactionwith different sulfonyl chlorides in dry DCM in the presence of a nonnucleophilic base like DIPEA followed by sequestering any remainingsulfonyl chloride by a polymer-supported quenching reagent liketris-(2-aminoethyl)-amine polystyrene (R. J. Booth, J. C. Hodges, J. Am.Chem. Soc. (1997) 119, 4882). Carbamates 9c (R. J. Booth, J. C. Hodges,J. Am. Chem. Soc. (1997) 119, 4882) are obtained by reactingchloroformates in dry DCM in the presence of a non nucleophilic baselike DIPEA, followed by sequestering any remaining chloroformate by apolymer-supported quenching reagent like tris-(2-aminoethyl)-aminepolystyrene. Thioureas 9d and ureas 9e were obtained after reaction withthio-isocyanates or isocyanates in DCM in the presence of a nonnucleophilic base like DIPEA, followed by sequestering any remainingthio-isocyanate or isocyanate by a polymer-supported quenching reagentlike tris-2-aminoethyl)-amine polystyrene (R. J. Booth, J. C. Hodges, J.Am. Chem. Soc. (1997) 119, 4882).

According to scheme 3b depicted in FIG. 3 b suitable protected amines 11bearing R₂, R₃, R₄, R₅, R₆, R₇, R₈, R₉ is allowed to react withdifferent reagents as described for scheme 3 a.

According to scheme 4 depicted in FIG. 4 suitable protected dipeptides 1bearing R₅, R₆, R₇ or 7 R₅, R₆, R₇, R₈, R₉ are coupled with a resin likeRink amide PEGA resin in the presence of a coupling reagent such asbenzotriazol-1-yloxytrispyrrolidinophosphonium hexafluorophosphate(PyBOP®), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride(EDCl), O-benzotriazol-1-yl-N,N,N′,N′-tetramethyluroniumhexafluorophosphate (HBTU), 1,3-dicyclohexylcarbodiimide (DCC), or thelike, in a suitable solvent (N-methylpyrrolidinone, DMF, DCK or thelike). Additionally an appropriate catalyst (e.g.,1-hydroxybenzotriazole (HOBT), 1-hydroxy-7-azabenzotriazole (HOAt), orthe like) and non-nucleophilic bases (e.g., N-methylmorpholine,triethylamine, N,N-diisopropylethylamine or the like, or any suitablecombination thereof) may be added. An example of a suitable protectinggroup for the amine function is the 9-fluorenylmethoxycarbonyl (Fmoc)group. This is followed by deprotection to give the free amine. Anexample of a suitable deprotection is piperidine in DMF. A suitableprotected building block bearing R₂, R₃, R₄ is then coupled in the sameconditions ad described before. Desired compounds 14 and 17 are obtainedafter deprotection of the amine function.

According to scheme 5a depicted in FIG. 5 a suitable protectedimmobilized amines 14 bearing R₂, R₃, R₄, R₅, R₆, R₇ are allowed toreact with different reagents. They can be reacted with acids, acylchlorides or anhydrides to provide the corresponding amides 14a. Anexample of standard coupling conditions with acids would be to combinewith HBTU and diisopropylethylamine in anhydrous DMF. Acyl chloride oranhydride would be reacted in dry DCM in the presence of a nonnucleophilic base like DIPEA (B. Raju, T. P. Kogan, Tetrahedron Lett.(1997) 38, 4965). Sulfonamide derivatives 14b are obtained afterreaction with differents sulfonyl chlorides in dry DCM in the presenceof DMAP (C. Gennari, B. Salom, D. Potenza, A. Williams, Angew. Chem.,Int. Ed. Engl. (1994) 33 2067). Carbamates 14c are obtained by reactingchloroformates in dry DCM in the presence of a non nucleophilic baselike DIPEA (T. Fukuyama, L. Li, A. A. Laird, R. K. Frank, J. Am. Chem.Soc. (1987) 109, 1587). Thioureas 14d and ureas 14e were obtained afterreaction with thio-isocyanates or isocyanates in DCM with or without anon nucleophilic base like DEPEA (P. C. Kearney, M. Fernandez, J. A.Flygare, J. Am. Chem. Soc. (1998) 63, 196).

According to scheme 5b depicted in FIG. 5 b suitable protectedimmobilized amines 17 bearing R₂, R₃, R₄, R₅, R₆, R₇, R₈, R₉ are allowedto react with different reagents as described for scheme 5 a.

According to scheme 6a depicted in FIG. 6 a suitable immobilizedderivatives 14 a-e bearing R₁, R₂, R₃, R₄, R₅, R₆, R₇ are cleaved fromthe resin to give the amides 18 a-e that are converted to thecorresponding nitrites 19 a-e by dehydration. An example of a suitablecleavage is TFA in DCM. The nitrites 19 a-e are also obtained directlyfrom the immobilized derivatives 14 a-e using trifluoroacetic anhydridefor the dehydration.

According to scheme 6b depicted in FIG. 6 b suitable immobilizedderivatives 17 a-e bearing R₁, R₂, R₃, R₄, R₅, R₆, R₇, R₅, R₉ arereacted to give the corresponding nitriles 21 a-e as described forscheme 6 a.

Method A: Coupling of Acyl Chlorides with Derivatized Amines inSolution.

Amine salt (1 eq) was dissolved in a mixture of 10% dry DMSO inanhydrous DCM, acyl chloride (1.5 eq) and diisopropylethylamine (2 eq)were added under Ar, and stirred for 2 h at room temperature.Tris-(2-aminoethyl)amine polystyrene (6 eq relative to excess acylchloride) and (polystyrylmethyl)trimethylammonium bicarbonate (4 eqrelative to expected amine salt) were added to the reaction mixture andagitated for 18 h at room temperature. The supernatant was separatedfrom the resin by filtration and the polymeric beads were washed withDCM and a mixture of DCM/MeOH (1/1) (three times). After evaporation ofthe solvent, the residue was dissolved/suspended in water andlyophilized to give the crude product.

Method E: Coupling of Anhydrides with Derivatized a Amines in Solution.

Amine salt (1 eq) was dissolved in a mixture of 10% dry DMSO inanhydrous DCM, anhydride (1.5 eq) and diisopropylethylamine (2 eq) wereadded under Ar, and stirred for 18 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (6 eq relative to excessanhydride) and (polystyrylmethyl)trimethylammonium bicarbonate (4 eqrelative to expected amine salt) were added to the reaction mixture andagitated for 18 h at room temperature. The supernatant was separatedfrom the resin by filtration and the polymeric beads were washed withDCM and a mixture of DCM/MeOH (1/1) (three times). After evaporation ofthe solvent, the residue was dissolved/suspended in water andlyophilized to give the crude product

Method C: Coupling of Chloroformates with Derivatized Amines inSolution.

Amine salt (1 eq) was dissolved in a mixture of 10% dry DMSO inanhydrous DCM, chloroformate (1.5 eq) and diisopropylethylamine (2 eq)were added under Ar, and stirred for 18 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (6 eq relative to excessanhydride) and (polystyrylmethyl)trimethylammonium bicarbonate (4 eqrelative to expected amine salt) were added to the reaction mixture andagitated for 18 h at room temperature. The supernatant was separatedfrom the resin by filtration and the polymeric beads were washed withDCM and a mixture of DC/MeOH (1/1) (three times). After evaporation ofthe solvent, the residue was dissolved/suspended in water andlyophilized to give the crude product

Method D: Coupling of Acids with Derivatized Amines in Solution.

Method D1: Coupling using 1-hydroxybenzotriazole-6-sulfonamidomethylpolystyrene

To a solution of PyBrOP (2 eq), acid (2 eq) and diisopropylethylamine (4eq) in anhydrous DMF was added1-hydroxybenzotriazole-6-sulfonamidomethyl polystyrene (2 eq). Themixture was reacted at room temperature for 5 h. After the firstactivation step the resin was washed with DMF (three times). The secondactivation step was performed under the same conditions as the firstone, and the resin was washed with DMF (five times).

The amine salt (1 eq) was added to a suspension of the resin inanhydrous DCM and diisopropylethylamine (2 eq). The polymer-boundactivated ester was reacted with this mixture at room temperature. After20 h, the supernatant was separated from the resin by filtration. Thepolymeric beads were washed with DCM and a mixture of DCM/MeOH (1/1)(three times), the solvent was removed under vacuum. The residue wasdissolved/suspended in water, and lyophilized to give the crude product.

Method D2: Coupling using N-cyclohexylcarbodiimide, N-methyl polystyrene

Amine salt (1 eq) and acid (1.5 eq) in a mixture of 10% dry DMSO inanhydrous DCM were stirred under Ar. After 10 minN-cyclohexylcarbodiimide, N′-methyl polystyrene (2 eq) was added. Thereaction was stirred overnight at room temperature. The supernatant wasseparated from the resin by filtration. The polymeric beads were washedwith DCM and a mixture of DCM/MeOH (1/1) (three times), the solvent wasremoved under vacuum The residue was dissolved/suspended in water andlyophilize to give the crude product.

Method D3: Coupling Using Standard Conditions for Peptides

To a solution of amine salt (1 eq) in anhydrous DMF was added the acid(1 eq), HBTU (1 eq) and Et₃N (2 eq). The reaction mixture was stirredovernight and then diluted with EtOAc. The organic phase was washed withsaturated aqueous solution of NaHCO₃ and saturated aqueous solution ofNaCl, dried over MgSO₄, filtered and evaporated. The residue waspurified by flash-chromatography.

Method E: Coupling of Sulfonyl Chlorides with Derivatized Amines inSolution.

Amine salt (1 eq) was dissolved in a mixture of 10% dry DMSO inanhydrous DCM, sulfonyl chloride (1.5 eq) and diisopropylethylamine (4eq) were added under Ar, and stirred 2 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (3 eq relative to excess sulfonylchloride) and (polystyrylmethyl)trimethylammonium bicarbonate (4 eqrelative to expected amine salt) were added to the reaction mixture andagitated for 18 h at room temperature. The supernatant was separatedfrom the resin by filtration, the polymeric beads were washed with DCMand a mixture of DCM/MeOH (1/1) (three times). After evaporation of thesolvent, the residue was dissolved/suspended in water and lyophilized togive the crude product

Method F: Coupling of Isocyanates with Derivatized Amines in Solution.

Amine salt (1 eq) was dissolved in a mixture of 10% dry DMSO inanhydrous DCM, isocyanate (1.5 eq) and diisopropylethylamine (2 eq) wereadded under Ar, and stirred for 2 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (3 eq relative to excessisocyanate) and (polystyrylmethyl)trimethylammonium bicarbonate (4 eqrelative to expected amine salt) were added to the reaction mixture andagitated for 18 h at room temperature. The supernatant was separatedfrom the resin by filtration, the polymeric beads were washed with DCMand a mixture of DC/MeOH (1/1) (three times). After evaporation of thesolvent, the residue was dissolved/suspended in water, and lyophilizedto give the crude product.

Method G: Coupling of Thioisocyanates with Derivatized Amines inSolution.

Amine salt (1 eq) was dissolved in a mixture of 10% dry DMSO inanhydrous DCM, thio-isocyanate (1.5 eq) and diisopropylethylamine (2 eq)were added under Ar, and stirred for 5 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (6 eq relative to excessthioisocyanate) and (polystyrylmethyl)trimethylammonium bicarbonate (4eq relative to expected amine salt) were added to the reaction mixtureand agitated for 18 h at room temperature The supernatant was separatedfrom the resin by filtration, the polymeric beads were washed with DCMand a mixture of DCM/MeOH (1/1) (three times). After evaporation of thesolvent, the residue was dissolved/suspended in water, and lyophilizedto give the crude product

Method H: Coupling of Acyl Chlorides with Derivatized Amines onSolid-Phase.

The immobilized amine (1 eq) was swollen in anhydrous DCM, acyl chloride(5 eq) and diisopropylethylamine (5 eq) were added, the mixture wasshaken 18 h at room temperature. The resin was filtered off and washedsuccessively with DNF, methanol, and dichloromethane and dried. Asolution of 50% trifluoroacetic acid in dichloromethane was added to theresin. The mixture was shaken 30 min at room temperature. Afterfiltration, the resin was washed with a solution of 50% trifluoroaceticacid in dichloromethane. After evaporation of the solvent, the residuewas dissolved/suspended in water, and lyophilized to give the crudeproduct.

Method I: Coupling of Anhydrides with Derivatized Amines on Solid-Phase.

The immobilized amine (1 eq) was swollen in anhydrous DCM, anhydride (5eq) and diisopropylethylamine (5 eq) were added, the mixture was shaken18 h at room temperature. The resin was filtered off and washedsuccessively with DMF, methanol, and dichloromethane and dried. Asolution of 50% trifluoroacetic acid in dichloromethane was added to theresin. The mixture was shaken 30 min at room temperature. Afterfiltration, the resin was washed with a solution of 50% trifluoroaceticacid in dichloromethane. After evaporation of the solvent, the residuewas dissolved/suspended in water, and lyophilized to give the crudeproducts.

Method J: Coupling of Chloroformates with Derivatized Amines onSolid-Phase.

The immobilized amine (1 eq) was swollen in anhydrous DCM, chloroformate(5 eq) and diisopropylethylamine (5 eq) were added, the mixture wasshaken 18 h at room temperature. The resin was filtered off and washedsuccessively with DMF, methanol, and dichloromethane and dried. Asolution of 50% trifluoroacetic acid in dichloromethane was added to theresin. The mixture was shaken 30 min at room temperature. Afterfiltration, the resin was washed with a solution of 50% trifluoroaceticacid in dichloromethane. After evaporation of the solvent, the residuewas dissolved/suspended in water, and lyophilized to give the crudeproducts.

Method K: Coupling of Acids with Derivatized Amines on Solid-Phase.

Acid (5 eq) was preactivated with HBTU (5 eq) and diisopropylethylamine(5 eq) in anhydrous DMF for 5 min, and added to the immobilized amine (1eq). The mixture was shaken 18 h at room temperature. The resin wasfiltered off and washed successively with DMF, methanol anddichloromethane and dried. A solution of 50% trifluoroacetic acid indichloromethane was added to the resin. The mixture was shaken 30 min atroom temperature. After filtration, the resin was washed with a solutionof 50% trifluoroacetic acid in dichloromethane. After evaporation of thesolvent, the residue was dissolved/suspended in water, and lyophilizedto give the crude product

Method L: Coupling of Sulfonyl Chlorides with Derivatized Amines onSolid-Phase.

The immobilized amine (1 eq) was swollen in anhydrous DCM, sulfonylchloride (5 eq) and DMF (5 eq) were added, the mixture was shaken 18 hat room temperature. The resin was filtered off and washed successivelywith DMF, methanol, and dichloromethane and dried. A solution of 50%trifluoroacetic acid in dichloromethane was added to the resin. Themixture was shaken 30 min at room temperature. After filtration, theresin was washed with a solution of 50% trifluoroacetic acid indichloromethane. After evaporation of the solvent, the residue wasdissolved/suspended in water, and lyophilized to give the crude product.

Method M: Coupling of Isocyanates with Derivatized Amines onSolid-Phase.

The immobilized amine (1 eq) was swollen in anhydrous DCM, isocyanate (5eq) was added and the mixture was shaken 18 h at room temperature. Theresin was filtered off and washed successively with DMF, methanol, anddichloromethane and dried. A solution of 50% trifluoroacetic acid indichloromethane was added to the resin. The mixture was shaken 30 min atroom temperature. After filtration, the resin was washed with a solutionof 50% trifluoroacetic acid in dichloromethane. After evaporation of thesolvent, the residue was dissolved/suspended in water, and lyophilizedto give the crude product.

Method N: Coupling of Thio-Isocyanates with Derivatized Amines onSolid-Phase.

The immobilized amine (1 eq) was swollen in anhydrous DCM,thio-isocyanate (5 eq) was added and the mixture was shaken 18 h at roomtemperature. The resin was filtered off and washed successively withDMF, methanol, and dichloromethane and dried. A solution of 50%trifluoroacetic acid in dichloromethane was added to the resin. Themixture was shaken 30 min at room temperature. After filtration, theresin was washed with a solution of 50% trifluoroacetic acid indichloromethane. After evaporation of the solvent, the residue wasdissolved/suspended in water, and lyophilized to give the crude product

Compounds were purified by HPLC.

EXAMPLE 2 2-Amino-3-naphthalen-2-yl-propionic acid cyanomethyl-amidetrifluoroacetate

To a solution of 3-aminoacetonitrile hydrogensulfate (1.61 g, 1.25 eq)in anhydrous DMF (36 mL) was added Boc-β-Nal-OH (3 g, 1 eq), HBTU (3.62g, 1 eq) and Et₃N (4 mL, 3.8 eq). The reaction mixture was stirredovernight and then diluted with EtOAc. The organic phase was washed withsaturated aqueous solutions of NaHCO₃ and NaCl, dried over MgSO₄,filtered and evaporated. The residue was purified byflash-chromatography hexane/ethyl acetate 3/2 to give[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidtert-butyl ester. The ester was dissolved in a solution of 50% TFA inDCM (15 mL), stirred at room temperature for 15 min and then evaporatedwith toluene. The residue was purified by HPLC to give2-amino-3-naphthalen-2-yl-propionic acid cyanomethyl-amidetrifluoroacetate (2.5 g, 70%).

EXAMPLE 3 [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamicacid tert-butyl ester

To a solution of 3-aminopropionitrile (146 μL, 1.25 eq) in anhydrous DMF(4.3 mL) was added Boc-β-Nal-OH (500 mg, 1 eq), HBTU (601.3 mg, 1 eq)and Et₃N (331.5 μL, 1.5 eq). The reaction mixture was stirred overnightand then diluted with EtOAc. The organic phase was washed with saturatedaqueous solutions of NaHCO₃ and NaCl, dried over MgSO₄, filtered andevaporated. The residue was purified by flash-chromatographyhexane/ethyl acetate 3/2 to give[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidtert-butyl ester (559 mg, 96%).

NMR-¹H (DMSO-d₆) δ=1.24 (s, 9H), 2.61 (m, 2H), 2.93 (dd, 1H, J=10.3,J=13.7 Hz, 1H), 3.13 (dd, 1H, J=4.3, J=13.7 Hz, 1H), 3.37 (m, 2H), 4.24(m, 1H), 6.99 (d, J=8.6 Hz, 1H), 7.43-7.50 (m, 3H), 7.73-7.87 (m, 3H),8.33 (m, 1H); MS: m/z: 367.8 [M⁺].

EXAMPLE 43-Naphthalen-2-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide

Amine salt (prepared as described in example 1) (10 mg) was dissolved ina mixture of 10% dry DMSO (100 μL) in anhydrous DCM (1 mL),4-trifluoromethylthio)-phenyl isocyanate (6.98 μL) anddiisopropylethylamine (10 μL) were added under Ar, and stirred for 2 hat room temperature. Tris-(2-aminoethyl)-amine polystyrene (10 mg) and(polystyrylmethyl) trimethylammonium bicarbonate (10 mg) were added tothe reaction mixture and agitated for 18 h at room temperature Thesupernatant was separated from the resin by filtration, the polymericbeads were washed with DCM and a mixture of DCM/MeOH (1/1) (threetimes). After evaporation of the solvent, the residue was was purifiedby HPLC to give3-naphthalen-2-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide (13.4 mg, 98%).

NMR-¹H (DMSO-d₆) δ3.06 (dd, 1H, J=7.7, J=13.7 Hz), 3.19 (dd, 1H, J=5.8,J=13.7 Hz), 4.18 (m, 2H), 4.60 (m, 1H), 7.38 (m, 1H), 7.43-7.52 (m, 4H),7.63 (m, 2H), 7.70 (s, 1H), 7.82-7.88 (m, 3H), 8.90 (m, 1H); MS: m/z:472.9 [M⁺].

EXAMPLE 5 3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide

Amine salt (prepared as described in example 1) (10 mg) was dissolved ina mixture of 10% dry DMSO (100 μL) in anhydrous DCM (1 mL), phenylisothiocyanate (5.20 μL) and diisopropylethylamine (10 μL) were addedunder Ar, and stirred for 5 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (10 mg) and(polystyrylmethyl)trimethylammonium bicarbonate (10 mg) were added tothe reaction mixture and agitated for 18 h at room temperature. Thesupernatant was separated from the resin by filtration, the polymericbeads were washed with DCM and a mixture of DCM/MeOH (1/1) (threetimes). After evaporation of the solvent, the residue was purified byHPLC to give 3-naphthalen-2-yl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide (10.5 mg, 93%).

NMR-¹H (DMSO-d₆) δ=3.21 (m, 1H), 3.29 (m, 1H), 4.18 (m, 2H), 5.26 (m,1H), 7.09 (m, 1H), 7.26 (m, 2H), 7.36 (m, 3H), 7.49 (m, 2H), 7.69 (s,1H), 7.82-7.90 (m, 3H), 8.92 (m, 1H), 9.82 (s, 1H); MS: m/z: 388.9 [M⁺].

EXAMPLE 63-Naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanomethyl amide

Amine salt (prepared as described in example 1) (10 mg) was dissolved ina mixture of 10% dry DMSO (100 μL) in anhydrous DCM (1 mL),4-tert-butyl-benzene-sulfonyl chloride (10.1 mg) anddiisopropylethylamine (20 μL) were added under Ar, and stirred 2 h atroom temperature. Tris-(2-aminoethyl)-amine polystyrene (10 mg) and(polystyrylmethyl)trimethylammonium bicarbonate (10 mg) were added tothe reaction mixture and agitated for 18 h at room temperature. Thesupernatant was separated from the resin by filtration, the polymericbeads were washed with DCM and a mixture of DCM/MeOH (1/1) (threetimes). After evaporation of the solvent, the residue was purified byHPLC to give3-naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanomethyl-amide (11.8 mg, 91%).

NMR-¹H (DMSO-4) δ=1.19 (s, 9H), 3.14 (m, 1H), 3.62 (m, 3H), 3.99 (m,2H), 7.13 (m, 1H), 7.18-7.38 (m, 5H), 7.46-7.52 (m, 3H), 7.61 (m, 1H),7.71-7.88 (m, 3H), 8.28 (m, 1H), 8.78 (m, 1H); MS: m/z: 450.2 [M⁺].

EXAMPLE 7 1-Methyl-cyclopropanecarboxylic acid [1-cyanomethylcarbamoyl)-2-naphthalen-2-yl-ethyl]-amide

To a solution of PyBrOP (148.5 mg), 1-methylcyclopropane carboxylic acid(33.4 mg) and diisopropylethylamine (152 μL) in anhydrous DMF (1.1 mL)was added 1-hydroxybenzotriazole-6-sulfonamidomethyl polystyrene (113.8mg). The mixture was reacted at room temperature for 5 h. After thefirst activation step the resin was washed with DMF (three times). Thesecond activation step was performed under the same conditions as thefirst one, and the resin was washed with DMF (five times).

The amine salt (prepared as described in example 1) (30 mg) was added toa suspension of the resin in anhydrous DCM (1 mL) anddiisopropylethylamine (152 μL). The polymer-bound activated ester wasreacted with this mixture at room temperature. After 20 h, thesupernatant was separated from the resin by filtration. The polymericbeads were washed with DCM and a mixture of DCM/MeOH (1/1) (threetimes). After evaporation of the solvent, the residue was purified byHPLC to give 1-methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-naphthlen-2-yl-ethyl]-amide (38.9 mg, 98%).

NMR-¹H (DMSO-d₆) δ=0.42 (m, 2H), 0.79 (m, 2H), 1.20 (s, 3H), 3.10 (dd,1H, J=9.8, J=13.6 Hz), 3.20 (dd, 1H, J=4.9, J=13.6 Hz, 1H), 4.16 (m,2H), 4.57 (m, 1H), 7.40-7.56 (m, 3H), 7.73 (s, 1H), 7.73-7.88 (m, 3H),8.66 (m, 1H); MS: m/z: 336.0 [M⁺].

EXAMPLE 84-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide

Amine salt (prepared as described in example 1) (30 mg) was dissolved ina mixture of 10% dry DMSO (100 μL) in anhydrous DCM (1 mL),4-(chloromethyl)benzoyl chloride (27 mg) and diisopropylethylamine (103mL) were added under Ar, and stirred for 2 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (40 mg) and(polystyrylmethyl)-trimethylammonium bicarbonate (40 mg) were added tothe reaction mixture and agitated for 18 h at room temperature. Thesupernatant was separated from the resin by filtration, the polymericbeads were washed with DCM and a mixture of DCM/MeOH (1/1) (threetimes). After evaporation of the solvent, the residue was purified byHPLC to give4-chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide(30.3 mg, 86%).

NMR-¹H (DMSO-d₆) δ=3.18 (m, 1H), 3.30 (m, 1H), 4.18 (m, 2H), 4.78 (s,2H), 4.83 (m, 1H), 7.40-7.62 (m, 5H), 7.78-7.85 (m, 6H), 8.82 (m, 1H);MS: m/z: 405.9 [M⁺].

EXAMPLE 9 N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-oxalamicacid methyl ester

Amine salt (prepared as described in example 1) (30 mg) was dissolved ina mixture of 10% dry DMSO (100 μL) in anhydrous DCM (1 mL), monomethyloxalyl chloride (14 μL) and diisopropylethylamine (103 μL) were addedunder Ar, and stirred for 2 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (40 mg) and(polystyrylmethyl)trimethylammonium bicarbonate (40 mg) were added tothe reaction mixture and agitated for 18 h at room temperature. Thesupernatant was separated from the resin by filtration, the polymericbeads were washed with DCM and a mixture of DCM/MeOH (1/1) (threetimes). After evaporation of the solvent, the residue was purified byHPLC to giveN-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-oxalamic acidmethyl ester (25.1 mg, 85%).

NMR-¹H (DMSO-4) δ=3.14 (dd, 1H, J=9.6, J=14.0 Hz, 1H), 3.29 (dd, 1H,J=4.9, J=14.0 Hz, 1H), 3.72 (s, 3H), 4.17 (m, 2H), 4.63 (m, 1H), 7.13(m, 1H), 7.40-7.49 (m, 3H), 7.73-7.87 (m, 4H), 8.84 (m, 1H), 9.14 (m,1H); MS: m/z: 340.0 [M⁺].

EXAMPLE 10N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic acid

Amine salt (prepared as described in example 1) (30 mg) was dissolved ina mixture of 10% dry DMSO (100 μL) in anhydrous DCM (1 mL), phthalicanhydride (21 mg) and diisopropylethylamine (103 μL) were added underAr, and stirred for 2 h at room temperature. Tris-(2-aminoethyl)-aminepolystyrene (40 mg) and (polystyrylmethyl)-trimethylammonium bicarbonate(40 mg) were added to the reaction mixture and agitated for 18 h at roomtemperature. The supernatant was separated from the resin by filtration,the polymeric beads were washed with DCM and a mixture of DCM/MeOH (1/1)(three times). After evaporation of the solvent, the residue waspurified by HPLC to giveN-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic acid(28.6 mg, 82%).

NMR-¹H (DMSO-d₆) δ=3.09 (dd, 1H, J=9.8, J=14.0 Hz, 1H), 3.35 (dd, 1H,J=5.1, J=14.0 Hz, 1H), 4.19 (m, 2H), 4.75 (m, 1H), 7.13 (m, 1H),7.45-7.51 (m, 5H), 7.72-7.87 (m, 5H), 8.55 (n, 1H), 8.79 (d, J=7.7 Hz,1H), 13.12 (bs, 1H); MS: m/z: 401.9 [M⁺].

EXAMPLE 11 [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamicacid ethyl ester

Amine salt (prepared as described in example 1) (30 mg) was dissolved ina mixture of 10% dry DMSO (100 μL) in anhydrous DCM (1 mL), ethylchloroformate (14 μL) and diisopropylethylamine (103 μL) were addedunder Ar, and stirred for 2 h at room temperature.Tris-(2-aminoethyl)-amine polystyrene (40 mg) was added to the reactionmixture and agitated for 18 h at room temperature. The supernatant wasseparated from the resin by filtration, the polymeric beads were washedwith DCM and a mixture of DCM/MEOH (1/1) (three times). Afterevaporation of the solvent, the residue was purified by HPLC to giveN-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic acid(25.5 mg, 90%).

NMR-¹H (DMSO-d₆) δ=1.04 (dd, 3 J=7.5, J=6.6 Hz H), 2.93 (dd, 1H, J=10.3,J=13.7 Hz, 1H), 3.14 (dd, 1H, J=4.5, J=13.7 Hz, 1H), 3.86 (m, 3H), 4.15(m, 2H), 4.30 (m, 1H), 7.43-7.51 (m, 3H), 7.75-7.88 (m, 4H), 8.76 (m,1H); MS: m/z: 326.0 [M⁺].

The following additional compounds of Formula I that can be prepared bythe methods described in this application.

Column A lists the different A substituents: Name A ¹H-NMR (DMSO-d₆,ppm) Methods MS Data

n = 1; 3-Naphthalen-2-yl-2-actylamino-propionic acid cyanomethyl-amide n= 2; 3-Naphthalen-2-yl-2-acetylamino-propionic acid cyanoethyl-amide A,B, H or I A, B, H or I m/z: 295.9 [M⁺]m/z: 309.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-pro- pionicacid cyanoethyl-amide F or M F or M m/z: 440.9 [M⁺]m/z: 454.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-urei-do]-propionic acid cyanomethyl-amide δ = 3.06(dd, 1H, J=7.7, J=13.7Hz),3.19(dd, 1H, J=5.8, J=13.7Hz), 4.18(m, 2H), 4.60(m, 1H), 7.38(m, 1H),7.43-7.52(m, 4H), 7.63(m, 2H), 7.70(s, 1H), 7.82-7.88(m, 3H), 8.90(m,1H). n = 2; 3-Naphthalen-2-yl-2-[3-(4-#trifluoromethylsulfanyl-phenyl)-urei- do]-propionic acidcyanoethyl-amide F or M F or M m/z: 472.9 [M⁺] m/z: 486.9 [M^(+ ])

n = 1; 3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-urei-do]-propionic acid cyanomethyl-amide δ = 3.08(dd, 1H, J=7.8, J=13.5Hz),3.16(dd, 1H, J=5.5, J=13.5Hz), 4.17(m, 2H), 4.59(m, 1H), 6.48(m, 1H),7.19(m, 2H), 7.28(m, 2H), 7.47-7.57(m, 3H), 7.70(s, 1H), 7.82-7.88(m,3H), 8.87(m, 1H). n = 2; 3-Naphthalen-2-yl-2-[3-(4-trifluoro#methoxy-phenyl)-urei- do]-propionic acid cyanoethyl-amide F or M F or Mm/z: 457.0 [M⁺] m/z: 471.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide F or M F or M m/z: 398.0 [M⁺]m/z: 412.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-benzyl-ureido)-propionic acidcyanomethyl-amide n = 2; 3-Naphthalen-2-yl-2-(3-benzyl-ureido)-propionicacid cyanoethyl-amide F or M F or M m/z: 387.0 [M⁺]m/z: 401.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(3-o-tolyl-ureido)-propionic acid cyanoethyl-amide For M F or M m/z: 387.0 [M⁺]m/z: 401.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-pro- pionicacid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 400.9 [M⁺]m/z: 414.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-pro- pionicacid cyanomethyl-amide. δ 2.00, 2.01(2s, 6H), 3.00(dd, 1H, J=8.2,J=13.3Hz), 3.17(dd, 1H, J=5.0, J=13.3Hz, 1H), 4.18(m, 2H), 4.60(m, 1H),6.97(s, 3H), 7.37(m, 1H), 7.49(m, 2H), 7.63(s, 1H), 7.79-7.88(m, 3H),8.84(m, 1H). n = 2;3-Naphthalen-2-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-pro- # pionic acidcyanoethyl-amide F or M F or M m/z: 401.0 [M⁺] m/z: 414.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(3-methyl-benzyl)-ureido]-pro- pionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(3-methyl-benzyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 401.0 [M⁺]m/z: 414.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-pro- pionicacid cyanoethyl-amide F or M F or M m/z: 408.9 [M⁺]m/z: 422.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 413.0 [M⁺]m/z: 427.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-pro- pionicacid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M E or K m/z: 413.1 [M⁺]m/z: 427.1 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 431.0 [M⁺]m/z: 445.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 449.1 [M⁺]m/z: 463.1 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-phenoxy-phenyl)-ureido]-pro- pionicacid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(4-phenoxy-phenyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 465.0 [M⁺]m/z: 479.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide F or M F or M m/z: 418.0 [M⁺]m/z: 432.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-cyclohexyl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(3-cyclohexyl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 378.9 [M⁺]m/z: 392.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-pro- pionicacid cyanomethyl-amide δ = 3.03(dd, 1H, J=7.5, J=13.9Hz, 1H), 3.16(dd,1H, J=5.5, J=13.9Hz, 1H), 4.16(m, 2H), 4.58(m, 1H), 5.91(s, 2H), 6.34(d,1H, J=8.4Hz, 1H), 6.60(dd, 1H, J=2.0, J=8.4Hz, 1H), 6.74(d, 1H, J=8.4Hz,1H), 7.09(d, 1H, J=2.0Hz, 1H), #7.37(m, 1H), 7.36-7.48(m, 2H), 7.70(s,1H), 7.81-7.88(m, 3H), 8.55(s, 1H), 8.84(m, 1H). n = 2;3-Naphthalen-2-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-pro- pionic acidcyanoethyl-amide F or M F or M m/z: #417.0 [M⁺] m/z: 431.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanoethyl-amide F or M F or M m/z: 405.0 [M⁺]m/z: 419.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-methyl-benzyl)-ureido]-pro- pionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(4-methyl-benzyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 401.0 [M⁺]m/z: 415.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-phenethyl-ureido)-ureido]-pro- pionic acidcyanomethyl-amide δ = 2.58(dd, 2H, J=7.2, J=7.4Hz), 2.93(dd, 1H, J=8.5,J=13.7Hz), 3.07(m, 1H), 3.14(m, 2H), 4.13(m, 1H), 4.49(m, 1H), 6.07(m,1H), 6.22(m, 1H), 7.11-7.26(m, 5H), 7.35(m, 1H), 7.47(m, 2H), 7.67(s,1H), 7.80-7.88(m, 3H), 8.73(m, #1H). n = 2;3-Naphthalen-2-yl-2-(3-phenethyl-ureido)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 401.0 [M⁺] m/z: 415.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-pro- pionicacid cyanoethyl-amide F or M F or M m/z: 463.0 [M⁺]m/z: 477.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(3-ethyl-thioureido)-propionic acid cyanoethyl-amideG or N G or N m/z: 340.9 [M⁺]m/z: 354.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(3-isopropyl-thioureido)-propionic acidcyanoethyl-amide G or N G or N m/z: 355.0 [M⁺]m/z: 369.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-thioureido]-pro- pionicacid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-thioureido]-pro- pionic acidcyanoethyl-amide G or N G or N m/z: 433.9 [M⁺]m/z: 447.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide δ = 3.21(m, 1H), 3.29(m, 1H), 4.18(m, 2H), 5.26(m,1H), 7.09(m, 1H), 7.26(m, 2H), 7.36(m, 3H), 7.49(m, 2H), 7.69(s, 1H),7.82-7.90(m, 3H), 8.92(m, 1H), 9.82(s, 1H). n = 2;3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionic acidcyanoethyl-amide G or #N G or N m/z: 388.9 [M⁺] m/z: 402.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-thio-ureido]-propionc acid cyanomethyl-amide δ = 3.20(m, 1H), 3.29(m, 1H),4.18(m, 2H), 5.25(m, 1H), 7.24(m, 2H), 7.38(m, 1H), 7.44-7.54(m, 4H),7.70(s, 1H), 7.82-7.90(m, 3H), 8.93(m, 1H), 9.92(s, 1H). n = 2;3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phen #yl)-thio-ureido]-propionic acid cyanoethyl-amide G or N G or N m/z: 472.9 [M⁺]m/z: 486.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thio-ureido}-propionic acid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thio-ureido}-propionic acid cyanoethyl-amide G or N G or N m/z: 456.9[M⁺]m/z: 470.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-[3-(4-methoxy-phenyl)-thioureido]-pro- pionicacid cyanomethyl-amide δ = 3.21(m, 1H), 3.29(m, 1H), 3.72(s, 3H),4.17(m, 2H), 5.25(m, 1H), 6.81(m, 1H), 7.16(m, 2H), 7.34(m, 1H), 7.49(m,2H), 7.66(s, 1H), 7.82-7.90(m, 3H), 8.86(m, 1H), 9.64(s, 1H). n = 2;3-Naphthalen-2-yl-2-[3-(4-methoxy-phenyl)-thio #ureido]-pro- pionic acidcyanoethyl-amide G or N G or N m/z: 419.0 [M⁺] m/z: 433.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic acidcyanomethyl-amide n = 2; 3-Naphthalen-2-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic acidcyanoethyl-amide E or L E or L m/z: #468.2 [M⁺] m/z: 482.2 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(thiophene-2-sulfonylamino)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(thiophene-2-sulfonylamino)-propionic acidcyanoethyl-amide E or L E or L m/z: 400.0 [M⁺]m/z: 414.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic acid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(4-trifluoromethoxy- benzenesulfonylamino)-propionicacid cyanoethyl-amide E or L E or L m/z: 478.1 [M⁺]m/z: 492.1 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-pro-pionic acid cyanomethyl-amide δ = 1.19(s, 9H), 3.14(m, 1H), 3.62(m, 3H),3.99(m, 2H), 7.13(m, 1H), 7.18-7.38(m, 5H), 7.46-7.52(m, 3H), 7.61(m,1H), 7.71-7.88(m, 3H), 8.28(m, 1H), 8.78(m, 1H). n = 2;3-Naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-pro- pionic acid#cyanoethyl-amide E or L E or L m/z: 450.2 [M⁺] m/z: 464.2 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(4-chloro-benzenesulfonylamino)-pro- pionicacid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(4-chloro-benzenesulfonylamino)-pro- pionic acidcyanoethyl-amide E or L E or L m/z: 428.1 [M⁺]m/z: 442.1 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(4-methoxy-benzenesulfonylamino)-pro- pionicacid cyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(4-methoxy-benzenesulfonylamino)-pro- pionic acidcyanoethyl-amide E or L E or L m/z: 424.1 [M⁺]m/z: 438.1 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide E or L E or L m/z: 445.2 [M⁺]m/z: 459.2 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-benzenesulfonylamino-propionic acidcyanomethyl-amide δ = 2.80(dd, 1H, J=9.2, J=13.5Hz), 3.02(dd, 1H, J=5.7,J=13.5Hz, 1H), 3.97(m, 2H), 4.03(m, 1H), 7.23(m, 3H), 7.37(m, 1H),7.45-7.51(m, 4H), 7.58(s, 1H), 7.70-7.85(m, 3H), 8.34(m, 1H). n = 2;3-Naphthalen-2-yl-2-benzenesulfonylamino)-propionic #acidcyanoethyl-amide E or L E or L m/z: 394.1 [M⁺] m/z: 408.1 [M⁺]

n = 1; 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanomethyl-carba-moyl)-2-naphthalen-2-yl-ethyl]-amide n = 2;1-Methyl-1H-indole-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide D or K D or K m/z: 411.1[M⁺]m/z: 425.0 [M⁺]

n = 1; 2-Propyl-pentanoic acid[1-(cyanomethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-amide n = 2; 2-Propyl-pentanoicacid[1-(cyanoethyl-carbamoyl)-2-naph- thalen-2-yl-ethyl]-amide D or K Dor K m/z: 380.1 [M⁺]m/z: 394.0 [M⁺]

n = 1; 1-Methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide δ= 0.42(m, 2H), 0.79(m, 2H),1.20(s, 3H), 3.10(dd, 1H, J=9.8, J=13.6Hz), 3.20(dd, 1H, J=4.9,J=13.6Hz, 1H), 4.16(m, 2H), 4.57(m, 1H), 7.40-7.56(m, 3H), 7.73(s, 1H),7.73-7.88(m, 3H), 8.66(m, 1H). n = 2; 1-Methyl-cyclopropanecarboxylic#acid[1-(cyanoethyl-carba- moyl)-2-naphthalen-2-yl-ethyl]-amide D or K Dor K m/z: 336.0 [M⁺] m/z: 350.0 [M⁺]

n = 1; Thiophene-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-amide n = 2; Thiophene-2-carboxylicacid[1-(cyanoethyl-carbamoyl)-2-naph- thalen-2-yl-ethyl]-amide D or K Dor K m/z: 363.9 [M⁺]m/z: 377.9 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-3-tri-fluoromethyl-benzamide n = 2;N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-3-tri-fluoromethyl-benzamide D or K D or K m/z: 425.9 [M⁺]m/z: 439.9 [M⁺]

n = 1; Biphenyl-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-amide n = 2; Biphenyl-2-carboxylicacid[1-(cyanoethyl-carbamoyl)-2-naph- thalen-2-yl-ethyl]-amide D or K Dor K m/z: 434.0 [M⁺]m/z: 448.0 [M^(+])

n = 1; 4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-benzamide n = 2;4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide D or K D or K m/z: 415.0 [M⁺]m/z: 429.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(2-1H-indol-3-yl-acetylamino)-pro- pionicacid cyanomethyl-amide δ = 2.99(dd, 1H, J=8.9, J=13.5Hz), 3.15(dd, 1H,J=5.1, J=13.5Hz), 3.51(s, 2H), 4.14(m, 2H), 4.59(m, 1H), 6.69(m, 1H),6.98(m, 1H), 7.07(s, 1H), 7.25(m, 2H), 7.35(m, 1H), 7.43-7.48(m, 2H),7.68(s, 1H), 7.75(m, 2H), 7.85(m, 1H), #8.29(m, 1H), 8.79(m, 1H). n = 2;3-Naphthalen-2-yl-2-(2-1H-indol-3-yl-acetylamino)-pro- pionic acidcyanoethyl-amide D or K D or K m/z: 411.1 [M⁺] m/z: 426.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(3-1H-indol-3-yl-propionylamino)-pro- pionicacid cyanomethyl-amide δ = 2.42(m, 2H), 2.74(m, 2H), 2.94(dd, 1H, J=9.3,J=13.7Hz), 3.15(m, 1H), 4.14(m, 2H), 4.64(m, 1H), 6.94(m, 1H), 7.01(m,2H), 7.10(m, 1H), 7.31(m, 1H), 7.38-7.49(m, 3H), 7.71(s, 1H), 7.79(m,2H), 7.86(m, 1H), 8.30(m, 1H), 8.75(m, 1H). n = 2;#3-Naphthalen-2-yl-2-(3-1H-indol-3-yl-rpopionylamino)-pro- pionic acidcyanoethyl-amide D or K D or K m/z: 425.0 [M⁺] m/z: 439.0 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-4-(1H-in-dol-3-yl)-butyramide δ = 1.70(m, 2H), 2.11(m, 2H), 2.47(m, 2H), 2.94(dd,1H, J=9.3, J=13.7Hz), 3.15(m, 1H), 4.14(m, 2H), 4.64(m, 1H), 6.92(m,2H), 7.03(m, 2H), 7.31(m, 1H), 7.37-7.49(m, 3H), 7.72(s, 1H),7.75-7.85(m, 4H), 8.22(m, 1H), 8.75(m, 1H). n = 2;#N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-4-(1H-in-dol-3-yl)-butyramide D or K D or K m/z: 493.0 [M⁺] m/z: 453.0 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benz- amiden = 2; N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benz- amideD or K D or K m/z: 358.0 [M⁺]m/z: 372.0 [M⁺]

n = 1; 3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-benzamide n = 2;3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-benzamide D or K D or K m/z: 406.0 [M⁺]m/z: 420.0[M⁺]

n = 1; 4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-benzamide δ = 3.18(m, 1H), 3.30(m, 1H), 4.18(m, 2H),4.78(s, 2H), 4.83(m, 1H), 7.40-7.62(m, 5H), 7.78-7.85(m, 6H), 8.82(m,1H). n = 2; 4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-naph-thalen-2-yl-ethyl]-benzamide D or #K D or K m/z: 405.9 [M⁺] m/z: 420.0[M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-fluoro-benzamide n = 2;N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-fluoro- benzamideD or K D or K m/z: 375.9 [M⁺]m/z: 389.9 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-nitro-benzamide n = 2;N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-nitro- benzamideD or K D or K m/z: 402.9 [M⁺]m/z: 416.9 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-acryl-amide n = 2;N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-acryl- amide D orK D or K m/z: 307.9 [M⁺]m/z: 321.9 [M⁺]

n = 1; 3-Naphthalen-2-yl-2,2-dimethyl-propionic acid cyanomethyl-amide n= 2; 3-Naphthalen-2-yl-2,2-dimethyl-propionic acid cyanoethyl- amide Dor K D or K m/z: 338.0 [M⁺]m/z: 352.0 [M⁺]

n = 1; 3-Naphthalen-2-yl-2-(2-methoxy-acetylamino)-propionic acidcyanomethyl-amide n = 2;3-Naphthalen-2-yl-2-(2-methoxy-acetylamino)-propionic acidcyanoethyl-amide D or K D or K m/z: 326.0 [M⁺]m/z: 340.0 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-eth- yl]-oxalamicacid methyl ester δ = 3.14(dd, 1H, J=9.6, J=14.0Hz), 3.29(dd, 1H, J=4.9,J=14.0Hz), 3.72(s, 3H), 4.17(m, 2H), 4.63(m, 1H), 7.13(m, 1H),7.40-7.49(m, 3H), 7.73-7.87(m, 4H), 8.84(m, 1H), 9.14(m, 1H). n = 2;#N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-eth- yl]-oxalamic acidmethyl ester m/z: 340.0 [M⁺] m/z: 354.0 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthala-mic acid δ = 3.09(dd, 1H, J=9.8, J=14.0Hz), 3.35(dd, 1H, J=5.1,J=14.0Hz), 4.19(m, 2H), 4.75(m, 1H), 7.13(m, 1H), 7.45-7.51(m, 5H),7.72-7.87(m, 5H), 8.55(m, 1H), 8.79(d, J=7.7Hz, 1H), 13.12(bs, 1H). n =2; #N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic acidB or I B or I m/z: 401.9 [M⁺] m/z: 415.9 [M⁺]

n = 1; N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-succinamicacid n = 2;N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-succinamic acid Bor I B or I m/z: 353.9 [M⁺]m/z: 367.9 [M⁺]

n = 1; 3-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl-carbamoyl]-acrylic acid n = 2;3-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl- carbamoyl]-acrylicacid B or I B or I m/z: 352.0 [M⁺]m/z: 366.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidisobutyl ester n = 2;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidisobutyl ester C or J C or J m/z: 354.0 [M⁺]m/z: 368.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidbutyl ester n = 1;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid butylester C or J C or J m/z: 354.0 [M⁺]m/z: 368.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidcyanomethyl ester n = 2;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidcyanomethyl ester C or J C or J m/z: 335.9 [M⁺]m/z: 349.9 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidbut-3-enyl ester n = 2;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidbut-3-enyl ester C or J C or J m/z: 352.0 [M⁺]m/z: 366.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester n = 2;[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester C or J C or J m/z: 436.0 [M⁺]m/z:450.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidhexyl ester n = 2;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid hexylester C or J C or J m/z: 382.0 [M⁺]m/z: 396.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidtert-butyl ester δ = 1.24(s, 9H), 2.93(dd, 1H, J=10.2, J=13.7Hz),3.14(dd, 1H, J=4.6, J=13.7Hz), 4.14(m, 2H), 4.27(m, 1H), 7.13(d, 1H,J=8.3Hz), 7.42-7.50(m, 3H), 7.72-7.87(m, 3H), 8.68(m, 1H). n = 2;#[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidtert-butyl ester δ = 1.24(s, 9H), 2.61(m, 2H), 2.93(dd, 1H, J=10.3,J=13.7Hz), 3.13(dd, 1H, J=4.3, J=13.7Hz), 3.37(m, 2H), 4.24(m, 1H),6.99(d, 1H, J=8.6Hz), 7.43-7.50(m, 3H), 7.73-7.87(m, 3H), 8.33(m, 1H).m/z: #353.9 [M⁺] m/z: 367.8 [M⁺]

n = 1; [1-(Cyanomethyl-carbmoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidmethyl ester n = 2;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid methylester C or J C or J m/z: 312.0 [M⁺]m/z: 326.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidethyl ester δ = 1.04(dd, 3H, J=7.5, J=6.6Hz), 2.93(dd, 1H, J=10.3,J=13.7Hz), 3.14(dd, 1H, J=4.5, J=13.7Hz), 3.86(m, 3H), 4.15(m, 2H),4.30(m, 1H), 7.43-7.51(m, 3H), 7.75-7.88(m, 4H), 8.76(m, 1H). n = 2;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid #ethylester C or J C or J m/z: 326.0 [M⁺] m/z: 340.0 [M⁺]

n = 1; [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid9H-fluoren-9-ylmethyl ester n = 2;[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid9H-fluoren-9-ylmethylester C or J C or J m/z: 475.9 [M⁺]m/z: 489.9 [M⁺]

Column A lists the different A substituents: Name A ¹H-NMR (DMSO-d₆,ppm) Methods MS Data

n = 1; 3-Benzo[b]thiophen-3-yl-2-acetylamino-propionic acidcyanomethyl-amide n = 2; 3-Benzo[b]thiophen-3-yl-2-acetylamino-propionicacid cyanoethyl-amide δ = 1.78(s, 3H), 2.60(m, 2H), 3.03(dd, 1H, J=9.3,J=14.7Hz), 3.22(m, 1H), 3.28(m, 2H), 4.58(m, 1H), 7.34-7.44(m, 3H),7.89-7.98(m, #2H), 8.22(m, 1H), 8.44(m, 1H). A, B, H or I A, B, H or Im/s 301.9 [M⁺]m/z: 315.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethyl-phenyl)-urei-do]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethyl-phenyl)-urei-do]-propionic acid cyanoethyl-amide F or M F or M m/z: 446.9 [M⁺]m/z:#460.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic acid cyanoethyl-amide F or M F or M m/z: 478.9[M⁺]m/z: #492.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-urei-do]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-urei-do]-propionic acid cyanoethyl-amide F or M F or M m/z: 463.0 [M⁺]m/z:477.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-cyano-phenyl)-ureido]-pro- pionicacid cyanomethyl-amide N = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-cyano-phenyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 404.0 [M⁺]m/z: 418.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-benzyl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-benzyl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 393.0 [M⁺]m/z: 407.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 393.0 [M⁺]m/z: 407.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-pro- pionicacid cyanoethyl-amide F or M F or M m/z: 406.9 [M⁺]m/z: 420.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(2,6-dimethyl-phenyl)-urei-do]-propionic acid cyanomethyl-amide. n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(2,6-dimethyl-phenyl)-urei- do]-propionicacid cyanoethyl-amide F or M F or M m/z: 407.0 [M⁺]m/z: 420.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(3-methyl-benzyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(3-methyl-benzyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 407.0 [M⁺]m/z: 420.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-urei-do]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-urei-do]-propionic acid cyanoethyl-amide F or M F or M m/z: 414.9 [M⁺]m/z:428.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 419.0 [M⁺]m/z: 433.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(2-phenyl-cyclopropyl)-urei-do]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(2-phenyl-cyclopropyl)-urei- do]-propionicacid cyanoethyl-amide F or M E or K m/z: 419.1 [M⁺]m/z: 433.1 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-adamantan-1-yl-ureido)-pro- pionicacid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-adamantan-1-yl-ureido)-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 437.0 [M⁺]m/z: 451.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-biphenyl-4-yl-ureido)-pro- pionicacid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-biphenyl-4-yl-ureido)-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 455.1 [M⁺]m/z: 469.1 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-phenoxy-phenyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-phenoxy-phenyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 471.0 [M⁺]m/z: 485.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-ureido]-pro- pionicacid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 424.0 [M⁺]m/z: 438.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-cyclohexyl-ureido)-propionic acidcyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-cyclohexyl-ureido)-propionic acidcyanoethyl-amide F or M F or M m/z: 384.9 [M⁺]m/z: 398.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-benzo[1,3]dioxol-5-yl-urei-do)-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-benzo[1,3]dioxol-5-yl-urei- do)-propionicacid cyanoethyl-amide F or M F or M m/z: 423.0 [M⁺]m/z: 437.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(2-fluoro-benzyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(2-fluoro-benzyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 411.0 [M⁺]m/z: 425.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-methyl-benzyl)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-methyl-benzyl)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 407.0 [M⁺]m/z: 421.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-phenethyl-ureido)-ureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-phenethyl-ureido)-ureido]-pro- pionic acidcyanoethyl-amide F or M F or M m/z: 407.0 [M⁺]m/z: 421.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(3,4,5-trimethoxy-phenyl)-urei-do]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(3,4,5-trimethoxy-phenyl)-urei-do]-propionic acid cyanoethyl-amide F or M F or M m/z: 469.0 [M⁺]m/z:483.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-ethyl-thioureido)-propionic acidcyanoethyl-amide G or N G or N m/z: 346.9 [M⁺]m/z: 360.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-isopropyl-thioureido)-pro- pionicacid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-isopropyl-thioureido)-pro- pionic acidcyanoethyl-amide G or N G or N m/z: 361.0 [M⁺]m/z: 375.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-thioureido]-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-thioureido]-pro- pionicacid cyanoethyl-amide G or N G or N m/z: 439.9 [M⁺]m/z: 453.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-phenyl-thioureido)-propionic acidcyanoethyl-amide G or N G or N m/z: 394.9 [M⁺]m/z: 408.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-thio-ureido]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-thio-ureido]-propionic acid cyanoethyl-amide G or N G or N m/z: 478.9[M⁺]m/z: 492.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phe-nyl]-thioureido}-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phe-nyl]-thioureido}-propionic acid cyanoethyl-amide G or N G or N m/z:462.9 [M⁺]m/z: #476.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-[3-(4-methoxy-phenyl)-thio-ureido]-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-[3-(4-methoxy-phenyl)-thio- ureido]-propionicacid cyanoethyl-amide G or N G or N m/z: 425.0 [M⁺]m/z: 439.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic acidcyanomethyl-amide n = 2; 3-Benzo[b]thiophen-3-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionic acidcyanoethyl-amide E or L E or L m/z: #474.2 [M⁺] m/z: 488.2 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(thiophene-2-sulfonylamino)-pro- pionicacid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(thiophene-2-sulfonylamino)-pro- pionic acidcyanoethyl-amide E or L E or L m/z: 406.0 [M⁺]m/z: 420.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(4-trilfuoromethoxy-benzenesulfonylamino)-propionic acid cyanoethyl-amide E or L E or L m/z:484.1 [M⁺]m/z: 498.1 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(4-tert-butyl- benzenesulfonylamino)-propionicacid cyanoethyl-amide E or L E or L m/z: 456.2 [M⁺]m/z: 470.2 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(4-chlorobenzene-sulfonylamino)-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(4-chloro-benzene- sulfonylamino)-propionicacid cyanoethyl-amide E or L E or L m/z: 434.1 [M⁺]m/z: 448.1 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(4-methoxy-benzenesulfonylamino)-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(4-methoxy- benzenesulfonylamino)-propionicacid cyanoethyl-amide E or L E or L m/s: 430.1 [M⁺]m/z: 444.1 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(quinoline-6-sulfonylamino)-pro- pionicacid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(quinoline-6-sulfonylamino)-pro- pionic acidcyanoethyl-amide E or L E or L m/z: 451.2 [M⁺]m/z: 465.2 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-benzenesulfonylamino-pro- pionic acidcyanomethyl-amide n = 2; 3-Benzo[b]thiophen-3-yl-2-benzenesulfonylamino-propionic acid cyanoethyl-amide E or L E or L m/z: 400.1 [M⁺]m/z: 414.1[M⁺]

n = 1; 1-Methyl-1H-indole-2-carboxylic acid[2-benzo[b]thio-phen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide n = 2;1-Methyl-1H-indole-2-carboxylic acid[2-benzo[b]thio-phen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide D or K D or K m/z: 417.1[M⁺]m/z: #431.0 [M⁺]

n = 1; 2-Propyl-pentanoic acid[2-benzo[b]thiophen-3-yl-1-(cyano-methyl-carbamoyl)-ethyl]-amide n = 2; 2-Propyl-pentanoicacid[2-benzo[b]thiophen-3-yl-1-(cyano- ethyl-carbamoyl)-ethyl]-amide Dor K D or K m/z: 386.1 [M⁺]m/z: 400.0 [M⁺]

n = 1; 1-Methyl-cyclopropanecarboxylic acid[2-ben-zo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide n = 2;1-Methyl-cyclopropanecarboxylic acid[2-ben-zo[b]thiphen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide D or K D or Km/z: 342.0 [M⁺]m/z: #356.0 [M⁺]

n = 1; Thiophene-2-carboxlic acid[2-benzo[b]thiophen-3-yl-1-(cyano-methyl-carbamoyl)-ethyl]-amide n = 2; Thiophene-2-carboxylicacid[2-benzo[b]thiophen-3-yl-1-(cyano- ethyl-carbamoyl)-ethyl]-amide Dor K D or K m/z: 369.9 [M⁺]m/z: 383.9 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-3-trifluoromethyl-benzamide n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth-yl]-3-trifluoromethyl-benzamide D or K D or K m/z: 431.9 [M⁺]m/z: 445.9[M⁺]

n = 1; Biphenyl-2-carboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyano-methyl-carbamoyl)-ethyl]-amide n = 2; Biphenyl-2-carboxylicacid[2-benzo[b]thiophen-3-yl-1-(cyano- ethyl-carbamoyl)-ethyl]-amide Dor K D or K m/z: 440.0 [M⁺]m/z: 454.0 [M⁺]

n = 1; 4-Acetylamino-N-[2-benzo[b]thiophen-3-yl-1-(cyano-methyl-carbamoyl)-ethyl]-benzamide n = 2;4-Acetylamino-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide D or K D or K m/z: 421.0 [M⁺]m/z: 435.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(2-1H-indol-3-yl-acetylamino)-pro-pionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(2-1H-indol-3-yl-acetylamino)-pro- pionic acidcyanoethyl-amide D or K D or K m/z: 417.1 [M⁺]m/z: 431.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(3-1H-indol-3-yl-pro-pionylamino)-propionic acid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(3-1H-indol-3-yl-pro- pionylamino)-propionicacid cyanoethyl-amide D or K D or K m/z: 431.0 [M⁺]m/z: 445.0 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-4-(1H-indol-3-yl)-butyramide n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth-yl]-4-(1H-indol-3-yl)-butyramide D or K D or K m/z: 445.0 [M⁺]m/z: 459.0[M⁺]

n = 1; n-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-benzamide n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth- yl]-benzamide Dor K D or K m/z: 364.0 [M⁺]m/z: 378.0 [M⁺]

n = 1; 3-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyano-methyl-carbamoyl)-ethyl]-benzamide n = 2;3-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carba-moyl)-ethyl]-benzamide D or K D or K m/z: 412.0 [M⁺]m/z: 426.0 [M⁺]

n = 1; 4-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyano-methyl-carbamoyl-ethyl]-benzamide n = 2;4-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carba-moyl-ethyl]-benzamide D or K D or K m/z: 411.9 [M⁺]m/z: 426.0 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-2-fluoro-benzamide n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth-yl]-2-fluoro-benzamide D or K D or K m/z: 381.9 [M⁺]m/z: 395.9 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-2-nitro-benzamide n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth-yl]-2-nitro-benzamide D or K D or K m/z: 408.9 [M⁺]m/z: 422.9 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-acrylamide n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth- yl]-acrylamideD or K D or K m/z: 313.9 [M⁺]m/z: 327.9 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2,2-dimethyl-propionic acidcyanomethyl-amide n = 2; 3-Benzo[b]thiophen-3-yl-2,2-dimethyl-propionicacid cyanoethyl-amide D or K D or K m/z: 344.0 [M⁺]m/z: 358.0 [M⁺]

n = 1; 3-Benzo[b]thiophen-3-yl-2-(2-methoxy-acetylamino)-pro- pionicacid cyanomethyl-amide n = 2;3-Benzo[b]thiophen-3-yl-2-(2-methoxy-acetylamino)-pro- pionic acidcyanoethyl-amide D or K D or K m/z: 332.0 [M⁺]m/z: 346.0 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-oxalamic acid methyl ester n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth- yl]-oxalamicacid methyl ester m/z: 346.0 [M⁺]m/z: 360.0 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-phthalamic acid n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth- yl]-phthalamicacid B or I B or I m/z: 407.9 [M⁺]m/z: 421.9 [M⁺]

n = 1; N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-succinamic acid n = 2;N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth- yl]-succinamicacid B or I B or I m/z: 359.9 [M⁺]m/z: 373.9 [M⁺]

n = 1; 3-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-ylcarbamoyl]-acrylic acid n = 2;3-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-eth-ylcarbamoyl]-acrylic acid B or I B or I m/z: 358.0 [M⁺]m/z: 372.0 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid isobutyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acidisobutyl ester C or J C or J m/z: 360.0 [M⁺]m/z: 374.0 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid butyl ester n = 1;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acidbutyl ester C or J C or J m/z: 360.0 [M⁺]m/z: 374.0 [M⁺]

n = 1; [2-Benzo[b]thiphen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid cyanomethyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acidcyanomethyl ester C or J C or J m/z: 341.9 [M⁺]m/z: 355.9 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid but-3-enyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acidbut-3-enyl ester C or J C or J m/z: 358.0 [M⁺]m/z: 372.0 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid 2-isopropyl-5-methyl-cyclohexyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acid2-isopropyl-5-methyl-cyclohexyl ester C or J C or J m/z: 442.0 [M⁺]m/z:#456.0 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid hexyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acidhexyl ester C or J C or J m/z: 388.0 [M⁺]m/z: 402.0 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid tert-butyl ester δ = 1.28(s, 9H), 3.05(dd, 1H, J=9.9,J=14.2Hz), 3.22(dd, 1H, J=4.6, J=14.2Hz), 4.15(m, 2H), 4.32(m, 1H),7.15(d, 1H, J=8.4Hz), 7.35-7.48(m, 3H), 7.89-7.98(m, 2H), 8.74(m, 1H). n= 2; #[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car-bamic acid tert-butyl ester δ = 1.29(s, 9H), 2.61(m, 2H), 3.04(m, 2H),3.22(m, 2H), 3.27-3.40(m, 4H), 4.28(m, 1H), 7.01(d, 1H, J=8.2Hz),7.40(m, 2H), 7.90(d, 1H, J=7.3Hz), 7.96(d, 1H, J=7.9Hz), 8.38(m, 1H).m/z: #359.9 [M⁺] m/z: 373.8 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid methyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acidmethyl ester C or J C or J m/z: 318.0 [M⁺]m/z: 332.0 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid ethyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acidethyl ester C or J C or J m/z: 332.0 [M⁺]m/z: 346.0 [M⁺]

n = 1; [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-eth-yl]-carbamic acid 9H-fluoren-9-ylmethyl ester n = 2;[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-car- bamic acid9H-fluoren-9-ylmethylester C or J C or J m/z: 481.9 [M⁺]m/z: 495.9 [M⁺]

EXAMPLE 12 Specificity of Inhibition of Certain Enzymes by CompoundsAccording to the Present Invention

In order to characterize the specificity of various compounds thefollowing assays were performed. PPIase activity of hPin1, hCyp18,LpCyp18, hFKBP12 and EcParvulin was measured using the protease-coupledPPIase assay according to Fischer et al. (Fischer, G.; Bang, H.; Mech,C. Determination of enzymatic catalysis fort he cis-trans-isomerizationof peptide binding in proline-containing peptides. [German] Diomed.Biochem. Acta 1984, 43, 1101-1111; Hennig et al., Selective Inactivationof Parvulin-like peptidyl-prolyl cis/trans isomerases by Juglon,Biochemistry. 1998, 37(17):5953-5960). For hPin1 measurementsAc-Ala-Ala-Ser(PO₃H₂)-Pro-Arg-pNA was used as a substrate and trypsin(final concentration 190 μg/ml) as an isomer-specific protease. Activitymeasurements of other PPIases were made with the substrate peptideSuc-Ala-Phe-Pro-Phe-pNA and the protease α-chymotrypsin (finalconcentration 470 μg/ml). The assays were performed in a final reactionvolume of 150 μL at final concentrations of 6 nM hPin1, 10 nM hCyp18, 5nM LpCyp18, 20 nM EcParvulin and 20 nM hFKBP12, respectively, and 120 μMsubstrate peptide in 35 mM HEPES (pH 7.8). For inhibition experiments100-0.01 μM of effector freshly diluted from a DMSO stock solution wereadded. The amount of solvent was kept constant within each experiment,usually below 0.3% (v/v). All reactions were started by addition ofprotease. The test was performed by observing the released4-nitroaniline at 390 nm with a MR500 UV/Vis spectrophotometer (Dynex)at 6° C. Data were evaluated by calculation of pseudo-first-order rateconstants k_(obs) in presence of PPIase and PPIase/effector,respectively, and corrected for the contribution of the non-catalyzedreaction (k₀). Inhibition constants IC₅₀ were calculated using SigmaPlot8.0 (SPSS).

The following target enzymes which are all rotamases belonging todifferent families of rotamases were used:

T-1: Protein interacting with NIMA (-kinase), hPin1

T-2: First described human Rapamycin receptor, hFKBP12

T-3: Human Cyclosporin A receptor with 18 kDa molecular weight, hCyp18

T4: Leishmonia pneumophila virulence Cyclosporin A receptor with 18 kDamolecular weight, LpCyp18

T-5: Bacterial Juglon sensitive non proteolytic enzyme, EcParv

These rotamases are known in the art. Their production andcharacteristics may be taken from the following references.

Review about all PPIase Families

Gothel, S. F.; Marahiel, M. A. II Peptidyl-prolyl cis-trans isomerases,a superfamily of ubiquitous folding catalysts [Review]. Cell. Molec.Life Sci. 1999, 55, 423-436

Pin1

Lu, K P.; Hanes, S. D.; Hunter, T. (1996) A human peptidyl-prolylisomerase essential for regulation of mitosis. Nature 1996, 380,544-547.

Yaffe, M. B.; Schutkowski, M.; Shen, M. H.; Zhou, X. Z.; Stukenberg, P.T.; Rahfeld, J. U.; Xu, J.; Kuang, J.; Kirschner, M. W.; Fischer, G.;Cantley, L. C.; Lu K P. Sequence-specific and phosphorylation-dependentpraline isomerization—A potential mitotic regulatory mechanism Science1997, 278, 1957-1960.

Shen, M.; Stukenberg, P. T.; Kirschner, M. W.; Lu, K P. The essentialmitotic peptidyl-prolyl isomerase Pin1 binds and regulatesmitosis-specific phosphoproteins. Genes Developm. 1998, 12, 706-720.

EcParvulin

Rahfeld J U. Schierhorn A. Mann K. Fischer G. A novel peptidyl-prolylcis/trans isomerase from Escherichia coli. FEBS Letters. 1994, 343,65-69

Rahfeld J U. Rucknagel K P. Schelbert B. Ludwig B. Hacker J. Mann KFischer G. Confirmation of the existence of a third family amongpeptidyl-prolyl cis/trans isomerases. Amino acid sequence andrecombinant production of parvulin. FEBS Letters. 1994, 352, 180-184

FKBPs (including FKBP12) and Cyclophilins (including Cyp18)

For recent reviews on cyclophilins and FKBPs and their effectors, see:(a) Fischer, G. Peptidyl-prolyl cis/trans isomerases and theireffectors. Angew. Chem., Int. Ed. Engl. 1994, 33, 1415-1436. (b) Galat,A.; Metcalfe, S. M. Peptidylproline cis/trans isomerases. Prog. Biophys.Molec. Biol. 1995, 63, 67-118.

LpCyp18

Schmidt B. Tradler T. Rahfeld J U. Ludwig B. Jain B. Mann K. Rucknagel KP. Janowski B. Schierhorn A. Kullertz G. Hacker J. Fischer G. Acyclophilin-like peptidyl-prolyl cis/trans isomerase from Legionellapneumophila-characterization, molecular cloning and overexpression. Mol.Microbiol. 1996, 21, 1147-1160

In order to cluster the various rotamase inhibitors the followingclasses were defined with “A” indicating the most potent rotamaseinhibitor.

A: IC₅₀<5 μM

B: 5 μM<IC₅₀<10 μM

C: 10 μM<IC₅₀<50 μM

D: 50 μM<IC₅₀<100 μM

E: IC₅₀>100 μM TABLE Specificity of the inhibition with rotamases TargetCompound N^(o) T-1 T-2 T-3 T-4 T-5

1 A E E E E

2 B E E E D

3 B E E E E

4 A E E E C

5 A E E E

6 B E E E

7 B E E E C

8 A E E E B

9 B E E E B

As may be taken from the above table the following compounds 1, 5, 8,are of class A and are thus extremely specific for hPin1.

The features of the present invention disclosed in the specification,the claims and/or the drawings may both separately and in anycombination thereof be material for realizing the invention in variousforms thereof.

1. A compound of formula (I):A-B-E-D  (I) wherein: A is selected from the group comprisingR^(a)-L1-K-L2-,

wherein the dashed lines indicate each and independently a single or adouble bond; wherein K is selected from the group comprising C=T, O, S,S(O) and S(O₂), or is absent, with =T being selected from the groupcomprising ═O, ═S, ═N—R¹, ═N<N, ═N—NO₂ and ═CH—NO₂, L1 and L2 are eachand independently selected from the group comprising O, S and amines,preferably NR², NR³; or being individually and independent from eachother absent; B is either present or absent, but if B is present then Bis

E is

whereby n is any integers from 1 to 5 whereby if n is 2 or more, any ofthe group(s) —(CR^(j)R^(k))— which are present, can be the same as ordifferent from any other of the group(s) —(CR^(j)R^(k))—, whereby anygroup —(CR^(j)R^(k))— is linked to any other group —(CR^(j)R^(k))— orany moiety of the compound through a bond, whereby the bond is selectedfrom the group comprising single bonds, double bonds and triple bonds; Dis selected from the group comprising —(CR¹R^(m))_(r)C(O)H,—(CR¹R^(m))_(r)C≡N, —(CR¹R^(m))_(r)NHNHC(O)NR⁵R⁶,—(CR¹R^(m))_(r)C(O)(CR^(n)R^(o))_(r′)C(O)OR⁷,—(CR¹R^(m))_(r)C(O)(CR^(n)R^(o))_(r′)C(O)NR⁸R⁹,—(CR¹R^(m))_(r′)CH(OH)(CR^(n)R^(o))_(r′)C(O)U, —(CR¹R^(m))_(r)C(O)W—(CR¹R^(m))_(r)C(O)CH₂W, —(CR¹R^(m))_(r)C(O)haloalkyl, and—(CR¹R^(m))_(r)C(O)(CR^(n)R^(o))_(r′)CHN₂, whereby U is —OR¹⁰ or—NR¹¹R¹², and W is —OR¹³, —SR¹⁴, —NR¹⁵R¹⁶, or a heterocyclic moiety,whereby r and r′ are any integers from 0 to 5 and any r and r′ mentionedare independently selected from any other r and r′ mentioned or present,whereby if r is 2 or more, any of the group(s) —(CR¹R^(m))— which arepresent, can be the same as or different from any of the other group(s)—(CR¹R^(m))—, whereby any group —(CR¹R^(m))— is linked to any othergroup —(CR¹R^(m))— or any moiety of the compound through a bond, wherebythe bond is selected from the group comprising single bonds, doublebonds and triple bonds, whereby if r′ is 2 or more, any of the group(s)—(CR^(n)R^(o))— which are present, can be the same as or different fromany of the other group(s) —(CR^(n)R^(o))—, whereby any group—(CR^(n)R^(o))— is linked to any other group —(CR^(n)R^(o))— or anymoiety of the compound through a bond, whereby the bond is selected fromthe group comprising single bonds, double bonds and triple bonds; Y isselected from the group comprising O, S, N—CN, N—NO₂, CH—NO₂ or NR¹⁷,wherein R¹⁷ is selected from the group comprising H, alkyl, substitutedalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, substitutedalkylcycloalkyl, aryl, substituted aryl, alkylaryl, substitutedalkylaryl, heterocyclyl, substituted heterocyclyl, alkylheterocyclyl,substituted alkylheterocyclyl, heteroaryl, substituted heteroaryl,alkylheteroaryl and substituted alkylheteroaryl; t is any integer from 1to 6, whereby if t is 2 or more, any of the group(s) —(CR^(d)R^(e))—which are present, can be the same as or different from any of the othergroup(s) —(CR^(d)R^(e))—, whereby any group —(CR^(d)R^(e))— is linked toany other group —(CR^(d)R^(e))— or any moiety of the compound through abond, whereby the bond is selected from the group comprising singlebonds, double bonds and triple bonds; Z is

, whereby R_(X) is selected from the group comprising amino acids,peptides, alkyl, substituted alkyl, straight alkyl, substituted straightalkyl, branched alkyl, substituted branched alkyl; or is absent; and Zis attached to any of the carbon of the cyclic structure; R^(a), R^(b),R^(c), R^(d), R^(e), R^(f), R^(g), R^(h), R^(i), R^(j), R^(k), R^(l),R^(m), R^(n) and R^(o) are each and independently from each otherselected from the group comprising H, OR¹⁸, SR¹⁹, NR²⁰R²¹, halo, alkyl,substituted alkyl, straight alkyl, substituted straight alkyl, branchedalkyl, substituted branched alkyl, straight alkenyl, substitutedstraight alkenyl, branched alkenyl, substituted branched alkenyl,straight alkynyl, substituted straight alkynyl, branched alkynyl,substituted branched alkynyl, cycloalkyl, substituted cycloalkyl,cycloalkenyl, substituted cycloalkenyl, heterocyclyl, substitutedheterocyclyl, mono-unsaturated heterocyclyl, poly-unsaturatedheterocyclyl, mono-substituted poly-unsaturated heterocyclyl,poly-substituted poly-unsaturated heterocyclyl, mono-substitutedmono-unsaturated heterocyclyl, poly-substituted mono-unsaturatedheterocyclyl, aryl, substituted aryl, heteroaryl and substitutedheteroaryl; or may be independently from each other absent; wherein,optionally, R^(d) and R^(f), R^(d) and R^(b), R^(d) and R^(c) are linkedso as to form a ring saturated or unsaturated comprising 4 to 12members, preferably 5 to 10 members; wherein R¹, R², R³ and R⁴ areselected from the group comprising H, alkyl, substituted alkyl,cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, substitutedalkylcycloalkyl, aryl, substituted aryl, alkylaryl, substitutedalkylaryl, heterocyclyl, substituted heterocyclyl, alkylheterocyclyl,substituted alkylheterocyclyl, heteroaryl, substituted heteroaryl,alkylheteroaryl and substituted alkylheteroaryl; and R⁵, R⁶, R⁷, R⁸, R⁹,R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁸, R¹⁹, R²⁰ and R²¹ are each andindependently selected from the group comprising H, alkyl, substitutedalkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, alkoxy,substituted alkoxy, aryloxy, substituted aryloxy, alkylamino,substituted alkylamino, arylamino and substituted arylamino; or is apharmaceutically acceptable salt or prodrug thereof.
 2. The compoundaccording to claim 1, wherein R^(b), R^(c), R^(d), R^(e), R^(f) andR^(g) are each and independently from each other selected from the groupcomprising H and alkyl, preferably lower alkyl.
 3. The compoundaccording to claim 1, wherein the dashed lines indicate a single bond.4. The compound according to claim 1, wherein K is selected from thegroup comprising C=T SO, S(O₂) with =T being ═O or ═S.
 5. The compoundaccording to claim 1, wherein L1 and L2 are each and independentlyselected from the group comprising NR² and NR³.
 6. The compoundaccording to claim 5, wherein R² and R³ are each and independentlyselected from the group comprising H and alkyl, preferably lower alkyl.7. The compound according to claim 1, wherein: A is selected from thegroup comprising

R²² is selected from the group comprising H, halogen, alkyl, cycloalkyl,aryl, heterocyclyl, heteroaryl and derivatives of any of these groups;and R²³, R^(23′), R^(23″) are each independently selected from the groupconsisting of H, alkyl, cycloalkyl, aryl, heteroaryl and heterocyclyland derivatives of any of these groups or is a pharmaceuticallyacceptable salt or prodrug thereof.
 8. The compound according to claim1, wherein Y is selected from the group comprising O, S and NR¹⁷, morepreferably selected from the group comprising O and S.
 9. The compoundaccording to claim 1, wherein R⁴ is selected from the group comprising Hand alkyl.
 10. The compound according to claim 9, wherein the alkyl is alower alkyl, preferably methyl.
 11. The compound according to claim 1,wherein n is 1 or
 2. 12. The compound according to claim 1, wherein E is

R²⁴, R²⁵, R²⁶, and R²⁷ are each individually and independently selectedfrom the group comprising H, halogen, alkyl, cycloalkyl, aryl,heterocyclyl, heteroaryl and derivatives of any of these groups.
 13. Thecompound according to claim 1, wherein if n=1, then r is different from0.
 14. The compound according to claim 1, wherein if n=2, then r is anyinteger from 0 to 5, preferably 0, 1 or
 2. 15. The compound according toclaim 1, wherein D is selected from the group comprising—(CH₂)_(r)C(O)H, —(CH₂)_(r)C≡N, —(CH₂)_(r)NHNHC(O)NR⁵R⁶,—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR⁷, —(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR⁸R⁹,—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W —(CH₂)_(r)C(O)CH₂W,—(CH₂)_(r)C(O)haloalkyl, and —(CH₂)_(r)C(O)(CH₂)_(r′)CHN₂; whereby U is—R¹⁰ or —NR¹¹R¹²; and W is —OR¹³, —SR¹⁴, —NR¹⁵R¹⁶, or a heterocyclicmoiety; whereby r and r′ is are any integers from 0 to 5 and any r andr′ mentioned are independently selected from any other r and r′mentioned or present and whereby any of R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹,R¹², R¹³, R¹⁴, R¹⁵, and R¹⁶ are each and independently selected from thegroup comprising H, alkyl, cycloalkyl, aryl, heteroaryl and heterocyclyland derivatives of any of these groups.
 16. The compound according toclaim 1, wherein D is —(CR¹R^(m))_(r)C≡N.
 17. The compound according toclaim 1, wherein t is 2, 3 or
 4. 18. A compound, preferably a compoundaccording to claim 1 having the structure of formula (I):A-B-E-D  (I) wherein: A is selected from the group comprising

B is either present or absent, but if B is present B is

E is

D is selected from the group comprising —(CH₂)_(r)C(O)H, —(CH₂)_(r)C≡N,—(CH₂)_(r)NHNHC(O)NR⁵R⁶, —(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR⁷,—(CH₂)_(r)C(O)(CH₂)_(r′)—C(O)NR⁸R⁹, —(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U,—(CH₂)_(r)C(O)W —CH₂)_(r)C(O)CH₂W, —(CH₂)_(r)C(O)haloalkyl, and—(CH₂)_(r)C(O)(CH₂)_(r′)CHN₂; whereby U is —OR¹⁰ or —NR¹¹R¹²; and W is—OR¹³, —SR¹⁴, —NR¹⁵R¹⁶, or a heterocyclic moiety; whereby r and r′ isare any integers from 0 to 5 and any r and r′ mentioned areindependently selected from any other r and r′ mentioned or present andwhereby any of R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵, and R¹⁶are each and independently selected from the group comprising-H, alkyl,cycloalkyl, aryl, heteroaryl and heterocyclyl and derivatives of any ofthese groups. Y is O, S, or NR¹⁷ wherein R¹⁷ is selected from the groupcomprising H, alkyl, cycloalkyl, aryl, heteroaryl and heterocyclyl andderivatives of any of these groups; t is 1, 2 or 3; Z is

, whereby R_(X) is selected from the group comprising amino acids,peptides and alkyl; R²², R^(h), R^(i), R²⁴, R²⁵, R²², and R²⁷ are eachindividually and independently selected from the group comprising H,halogen, alkyl, cycloalkyl, aryl, heterocyclyl, heteroaryl andderivatives of any of these groups; R²³, R^(23′), R^(23″), R⁴ are eachindependently selected from the group consisting of H, alkyl,cycloalkyl, aryl, heteroaryl and heterocyclyl and derivatives of any ofthese groups or is a pharmaceutically acceptable salt or prodrugthereof.
 19. The compound according to claim 1, wherein each R²², R^(h),R^(i), R⁴, R²⁴, R²⁵, R²⁶, and R²⁷ is individually and independently aderivative of any of alkyl, cycloalkyl, aryl, heterocyclyl, orheteroaryl, whereby any of these groups is individually andindependently substituted by one or more groups of the formula R²⁸,whereby R²⁸ is selected from the group comprising alkyl, cycloalkyl,aryl, heterocyclyl, heteroaryl, alkoxy, aryloxy, arylalkoxy,alkoxycarbonyl, aryloxycarbonyl, alkanoyl, aroyl, alkanoyloxy, aroyloxy,carbamoyl, carbamoyl derivative, alkanoylamino, aroylamino, alkylthio,alkylthio derivatives, arylthio, arylthio derivatives, ureido, ureidoderivatives, alkoxycarbonylamino, aryloxycarbonylamino,alkylcarbamoyloxy, arylcarbamoyloxy, alkylsulfonylamino,arylsulfonylamino, alkylaminosulfonyl, arylaminosulfonyl, amino, aminoderivatives and preferably R²⁸ is further substituted by one or moreR²⁹, whereby R²⁹ is selected from the group comprising alkyl,cycloalkyl, aryl, arylalkyl, alkoxy, aryloxy, arylalkoxy, alkanoyl,aroyl, amino, halogen, hydroxy, oxo, carboxy, cyano, nitro, amidino andguanidino.
 20. The compound according to claim 19, wherein the carbamoylgroup is derivatized, preferably the nitrogen atom may be independentlymono- or di-substituted by alkyl, aryl, heterocyclyl or heteroaryl;and/or the alkylthio group is derivatized, preferably the sulfur atom isoxidized to a sulfoxide or sulfone; and/or the arylthio group isderivatized, preferably the sulfur atom is oxidized to a sulfoxide orsulfone; and/or the ureido group is derivatized, preferably either thenitrogen atom is independentllty mono- or di-substituted by a groupwhich is selected from the group comprising alkyl, aryl, heterocyclyl orheteroaryl, alkoxycarbonylamino, aryloxycarbonylamino,alkyllycarbamoyloxy, arylcarbamoyloxy, alkylsulfonylamino,arylsulfonylamino, alkylaminosulfonyl, arylaminosulfonyl; and/or theamino group is derivatized, preferably the nitrogen atom isindependently mono- or di-substituted by alkyl, aryl, heterocyclyl orheteroaryl, halogen, hydroxy, oxo, carboxy, cyano, nitro, amidino andguanidino.
 21. The compound according to claim 1, wherein B is presentand has the meaning as defined in any of the preceding claims, E is

with R²⁴ to R²⁷ having the meaning as defined in any of the precedingclaims.
 22. The compound according to claim 1, wherein D is selectedfrom the group comprising —(CH₂)_(r)C(O)H, —(CH₂)_(r)C≡N,—(CH₂)_(r)NHNHC(O)NR⁵R⁶, —C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR⁷,—(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR⁸R⁹, —(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U,—(CH₂)_(r)C(O)W, whereby U is —OR¹⁰ or —NR¹¹R¹²; and W is —OR¹³, —SR¹⁴,—NR¹⁵R¹⁶, or a heterocyclic moiety; whereby r and r′ is are any integersfrom 0 to 5 and any of R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵,and R¹⁶ are each and independently selected from the group comprising H,alkyl, phenyl, benzyl, and phenethyl.
 23. The compound according toclaim 22, wherein D is —(CH₂)_(r)C≡N and r is any integer from 0 to 3.24. The compound according to claim 1, wherein B is


25. The compound according to claim 24, wherein D is selected from thegroup comprising —(CH₂)_(r)C(O)H, —(CH₂)_(r)C≡N,—(CH₂)_(r)NHNHC(O)NR⁵R⁵R⁶, —C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR⁷,—(CH₂)_(r′)C(O)(CH₂)_(r′)C(O)NR⁸R⁹, —(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U,—(CH₂)_(r)C(O)W, whereby U is —OR¹⁰ or —NR¹¹R¹²; and W is —OR¹³, —SR¹⁴,—NR¹⁵R¹⁶, or a heterocyclic moiety; whereby r and r′ are any integersfrom 0 to 5 and any of R⁵, R⁶, R⁷, R⁸, R⁹, R⁹, R¹⁰, R¹¹, R¹¹, R¹², R¹³,R¹⁴, R¹⁵, and R¹⁶ are each and independently selected from the groupcomprising H, alkyl, phenyl, benzyl, and phenethyl.
 26. The compoundaccording to claim 25, wherein D is —(CH₂)_(r)C≡N and r is any integerfrom 0 to
 3. 27. The compound according to claim 1, wherein A is

or a pharmaceutically acceptable salt or prodrug thereof.
 28. Thecompound according to claim 27, wherein D is selected from the groupcomprising —(CH₂)_(r)C(O)H, —(CH₂)_(r)C≡N, —(CH₂)_(r)NHNHC(O)NR⁵R⁶,—C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR⁷, —(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR⁸R⁹,—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W, whereby U is —OR¹⁰ or—NR¹⁰R¹²; and W is —OR¹³, —SR¹⁴, —NR¹⁵R¹⁶, or a heterocyclic moiety;whereby r and r′ are any integers from 0 to 5 and any of R⁵, R⁶, R⁷, R⁸,R⁹, R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵, and R¹⁶ are each and independentlyselected from the group comprising H, alkyl, phenyl, benzyl, andphenethyl.
 29. The compound according to claim 28, wherein D is—(CH₂)_(r)C≡N and r is any integer from 0 to
 3. 30. The compoundaccording to claim 1, wherein B is absent and wherein the other residueshave the same meaning as given in claim
 1. 31. The compound according toclaim 30, wherein D is selected from the group comprising—(CH₂)_(r)C(O)H, —(CH₂)_(r)C≡N, —(CH₂)_(r)NHNHC(O)NR⁵R⁶,—C(CH₂)_(r)C(O)(CH₂)_(r′)C(O)OR⁷, —(CH₂)_(r)C(O)(CH₂)_(r′)C(O)NR⁸R⁹,—(CH₂)_(r)CH(OH)(CH₂)_(r′)C(O)U, —(CH₂)_(r)C(O)W, whereby U is —OR¹⁰ or—NR¹¹R¹²; and W is —OR¹³, —SR¹⁴, —NR¹⁵R¹⁶, or a heterocyclic moiety;whereby r and r′ are any integers from 0 to 5 and any of R⁵, R⁶, R⁷, R⁸,R⁹, R¹⁰, R¹, R¹², R¹³, R¹⁴, R¹⁵, and R¹⁶ are each and independentlyselected from the group comprising H, alkyl, phenyl, benzyl, andphenethyl.
 32. The compound according to claim 31, wherein D is—(CH₂)_(r)C≡N and r is any integer from 0 to
 3. 33. The compoundaccording to claim 1, whereby the compound is selected from the groupcomprising: 3-(1H-Indol-3-yl)-2-acetylamino-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-(1H-Indol-3-yl)-2-(3-benzyl-ureido)-propionic acidcyanomethyl-amide, 3-(1H-Indol-3-yl)-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-(1H-Indol-3-yl)-2-(3-cyclohexyl-ureido)-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-(1H-Indol-3-yl)-2-(3-ethyl-thioureido)-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-(1H-Indol-3-yl)-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-(thiophene-2-sulfonylamino)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide, 3-(1H-Indol-3-yl)-2-benzenesulfonylamino-propionicacid cyanomethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,3-(1H-Indol-3-yl)-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-2-fluoro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-2-nitro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-acrylamide,3-(1H-Indol-3-yl)-2,2-dimethyl-propionic acid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-(2-methoxy-acetylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-phthalamic acid,N-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-succinamic acid,3-[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-acrylicacid, [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidisobutyl ester,[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidhexyl ester,[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid methylester, [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidethyl ester,[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid9H-fluoren-9-ylmethyl ester, 3-(1H-Indol-3-yl)-2-acetylamino-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-(1H-Indol-3-yl)-2-(3-benzyl-ureido)-propionic acidcyanoethyl-amide, 3-(1H-Indol-3-yl)-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(3-adamantan-1-yl-ureido)-propionic acidcyanoethyl-amide, 3-(1H-Indol-3-yl)-2-(3-biphenyl-4-yl-ureido)-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-(1H-Indol-3-yl)-2-(3-cyclohexyl-ureido)-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-(1H-Indol-3-yl)-2-(3-ethyl-thioureido)-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-(3-isopropyl-thioureido)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanoethyl-amide, 3-(1H-Indol-3-yl)-2-(3-phenyl-thioureido)-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-(thiophene-2-sulfonylamino)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide, 3-(1H-Indol-3-yl)-2-benzenesulfonylamino-propionicacid cyanoethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide2-Propyl-pentanoic acid[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-amide,4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,3-(1H-indol-3-yl)-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanoethyl-amide,3-(1H-Indol-3-yl)-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-2-fluoro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-2-nitro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-acrylamide,3-(1H-Indol-3-yl)-2,2-dimethyl-propionic acid cyanoethyl-amide,3-(1H-Indol-3-yl)-2-(2-methoxy-acetylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-phthalamic acid,N-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-succinamic acid,3-[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-acrylicacid, [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidisobutyl ester,[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanomethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid hexylester, [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid methylester, [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acidethyl ester, [1-(Cyanoethyl-carbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamicacid 9H-fluoren-9-ylmethylester,3-(4-Hydroxy-phenyl)-2-acetylamino-propionic acid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-(4-Hydroxy-phenyl)-2-(3-benzyl-ureido)-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-cyclohexyl-ureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(thiophene-2-sulfonylamino)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-tert-butyl-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide, 3-(4-Hydroxy-phenyl)-2-benzenesulfonylamino-propionicacid cyanomethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,3-(4-Hydroxy-phenyl)-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-fluoro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-nitro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-acrylamide,3-(4-Hydroxy-phenyl)-2,2-dimethyl-propionic acid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(2-methoxy-acetylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-phthalamicacid,N-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-succinamicacid,3-[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethylcarbamoyl]-acrylicacid, [1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamicacid isobutyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidbutyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidhexyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidmethyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidethyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid9H-fluoren-9-ylmethyl ester,3-(4-Hydroxy-phenyl)-2-acetylamino-propionic acid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-(4-Hydroxy-phenyl)-2-(3-benzyl-ureido)-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-adamantan-1-yl-ureido)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-(4-Hydroxy-phenyl)-2-(3-cyclohexyl-ureido)-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-ethyl-thioureido)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-isopropyl-thioureido)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanoethyl-amide, 3-(4-Hydroxy-phenyl)-2-(3-phenyl-thioureido)-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(thiophene-2-sulfonylamino)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-tert-butyl-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide, 3-(4-Hydroxy-phenyl)-2-benzenesulfonylamino-propionicacid cyanoethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-amide,4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,3-(4-hydroxy-phenyl)-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,41-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-fluoro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-2-nitro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-acrylamide,3-(4-Hydroxy-phenyl)-2,2-dimethyl-propionic acid cyanoethyl-amide,3-(4-Hydroxy-phenyl)-2-(2-methoxy-acetylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-phthalamic acid,N-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-succinamic acid,3-[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethylcarbamoyl]-acrylicacid, [1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamicacid isobutyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidbutyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanomethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidhexyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidmethyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acidethyl ester,[1-(Cyanoethyl-carbamoyl)-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid9H-fluoren-9-ylmethylester, 3-Phenyl-2-acetylamino-propionic acidcyanomethyl-amide,3-Phenyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Phenyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Phenyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-benzyl-ureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionicacid cyanomethyl-amide,3-Phenyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Phenyl-2-[3-(3-methyl-benzyl)-ureido]-propionicacid cyanomethyl-amide,3-Phenyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide,3-Phenyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide, 3-Phenyl-2-[3-(4-nitro-phenyl)-ureido]-propionicacid cyanomethyl-amide, 3-Phenyl-2-(3-cyclohexyl-ureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionicacid cyanomethyl-amide,3-Phenyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide, 3-Phenyl-2-[3-(4-methyl-benzyl)-ureido]-propionicacid cyanomethyl-amide,3-Phenyl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanomethyl-amide,3-Phenyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-[3-(4-nitro-phenyl)-thioureido]-propionicacid cyanomethyl-amide, 3-Phenyl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide,3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Phenyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Phenyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Phenyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanomethyl-amide, 3-Phenyl-2-(thiophene-2-sulfonylamino)-propionicacid cyanomethyl-amide,3-Phenyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Phenyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(4-chloro-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-Phenyl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide, 3-Phenyl-2-benzenesulfonylamino-propionic acidcyanomethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide, 2-Propyl-pentanoicacid [1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide, Thiophene-2-carboxylicacid [1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-amide,4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,3-Phenyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-1H-indol-3-yl-propionylamino)-propionicacid cyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-2-nitro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-acrylamide,3-Phenyl-2,2-dimethyl-propionic acid cyanomethyl-amide,3-Phenyl-2-(2-methoxy-acetylamino)-propionic acid cyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-oxalamic acid methyl ester,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-phthalamic acid,N-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-succinamic acid,3-[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethylcarbamoyl]-acrylic acid,[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid isobutyl ester,[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid butyl ester,[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid hexyl ester,[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid tert-butylester, [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid methylester, [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid ethylester, [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid9H-fluoren-9-ylmethyl ester, 3-Phenyl-2-acetylamino-propionic acidcyanoethyl-amide,3-Phenyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide3-Phenyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Phenyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-benzyl-ureido)-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide, 3-Phenyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionicacid cyanoethyl-amide,3-Phenyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Phenyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Phenyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide, 3-Phenyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionicacid cyanoethyl-amide, 3-Phenyl-2-(3-adamantan-1-yl-ureido)-propionicacid cyanoethyl-amide, 3-Phenyl-2-(3-biphenyl-4-yl-ureido)-propionicacid cyanoethyl-amide,3-Phenyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Phenyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-cyclohexyl-ureido)-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionicacid cyanoethyl-amide, 3-Phenyl-2-[3-(2-fluoro-benzyl)-ureido]-propionicacid cyanoethyl-amide, 3-Phenyl-2-[3-(4-methyl-benzyl)-ureido]-propionicacid cyanoethyl-amide, 3-Phenyl-2-(3-phenethyl-ureido)-ureido]-propionicacid cyanoethyl-amide,3-Phenyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-ethyl-thioureido)-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-isopropyl-thioureido)-propionic acidcyanoethyl-amide, 3-Phenyl-2-[3-(4-nitro-phenyl)-thioureido]-propionicacid cyanoethyl-amide, 3-Phenyl-2-(3-phenyl-thioureido)-propionic acidcyanoethyl-amide,3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-Phenyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanoethyl-amide,3-Phenyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-Phenyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanoethyl-amide, 3-Phenyl-2-(thiophene-2-sulfonylamino)-propionicacid cyanoethyl-amide,3-Phenyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Phenyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanoethyl-amide, 3-Phenyl-2-(4-chloro-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-Phenyl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanoethyl-amide, 3-Phenyl-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide, 3-Phenyl-2-benzenesulfonylamino-propionic acidcyanoethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide, 2-Propyl-pentanoic acid[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide, Thiophene-2-carboxylicacid [1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-amide,4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,3-Phenyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanoethyl-amide, 3-Phenyl-2-(3-1H-indol-3-yl-propionylamino)-propionicacid cyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-phenyl-ethyl]-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-2-nitro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-acrylamide,3-Phenyl-2,2-dimethyl-propionic acid cyanoethyl-amide,3-Phenyl-2-(2-methoxy-acetylamino)-propionic acid cyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-oxalamic acid methyl ester,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-phthalamic acid,N-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-succinamic acid,3-[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethylcarbamoyl]-acrylic acid,[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid isobutyl ester,[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid butyl ester,[1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid cyanomethylester, [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acidcyanomethyl ester, [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamicacid but-3-enyl ester,[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid but-3-enylester, [1-(Cyanomethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid hexyl ester,[1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid tert-butylester, [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid methylester, [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid ethylester, [1-(Cyanoethyl-carbamoyl)-2-phenyl-ethyl]-carbamic acid9H-fluoren-9-ylmethylester, 3-Methylsulfanyl-2-acetylamino-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-benzyl-ureido)-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-indan-5-yl-ureido)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-biphenyl-4-yl-ureido)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-cyclohexyl-ureido)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-ethyl-thioureido)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-(thiophene-2-sulfonylamino)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-benzenesulfonylamino-propionicacid cyanomethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,3-Methylsulfanyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanomethyl-amide,3-Methylsulfanyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-nitro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-acrylamide,3-Methylsulfanyl-2,2-dimethyl-propionic acid cyanomethyl-amide,3-Methylsulfanyl-2-(2-methoxy-acetylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-phthalamic acid,N-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-succinamic acid,3-[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethylcarbamoyl]-acrylicacid, [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidisobutyl ester,[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidhexyl ester, [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamicacid tert-butyl ester,[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid methylester, [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidethyl ester, [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamicacid 9H-fluoren-9-ylmethyl ester,3-Methylsulfanyl-2-acetylamino-propionic acid cyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-benzyl-ureido)-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido)-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-indan-5-yl-ureido)-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-adamantan-1-yl-ureido)-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-cyclohexyl-ureido)-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-ethyl-thioureido)-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-isopropyl-thioureido)-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-(3-phenyl-thioureido)-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-(thiophene-2-sulfonylamino)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-Methylsulfanyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide, 3-Methylsulfanyl-2-benzenesulfonylamino-propionic acidcyanoethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-amide,4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,3-Methylsulfanyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanoethyl-amide,3-Methylsulfanyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-2-nitro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-acrylamide,3-Methylsulfanyl-2,2-dimethyl-propionic acid cyanoethyl-amide,3-Methylsulfanyl-2-(2-methoxy-acetylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-oxalamic acid methylester, N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-phthalamicacid, N-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-succinamicacid,3-[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethylcarbamoyl]-acrylicacid, [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidisobutyl ester,[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanomethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid hexylester, [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acid methylester, [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamic acidethyl ester, [1-(Cyanoethyl-carbamoyl)-2-methylsulfanyl-ethyl]-carbamicacid 9H-fluoren-9-ylmethylester,3-Methanesulfonyl-2-acetylamino-propionic acid cyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Methanesulfonyl-2-(3-benzyl-ureido)-propionic acidcyanomethyl-amide, 3-Methanesulfonyl-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Methanesulfonyl-2-(3-cyclohexyl-ureido)-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Methanesulfonyl-2-(3-ethyl-thioureido)-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-Methanesulfonyl-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-3-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-(thiophene-2-sulfonylamino)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide, 3-Methanesulfonyl-2-benzenesulfonylamino-propionicacid cyanomethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,3-Methanesulfonyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-nitro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-acrylamide,3-Methanesulfonyl-2,2-dimethyl-propionic acid cyanomethyl-amide,3-Methanesulfonyl-2-(2-methoxy-acetylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-phthalamic acid,N-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-succinamic acid,3-[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethylcarbamoyl]-acrylicacid, [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidisobutyl ester,[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidhexyl ester,[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid methylester, [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidethyl ester,[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid9H-fluoren-9-ylmethyl ester, 3-Methanesulfonyl-2-acetylamino-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Methanesulfonyl-2-(3-benzyl-ureido)-propionic acidcyanoethyl-amide, 3-Methanesulfonyl-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanoethyl-amide, 3-Methanesulfonyl-2-(3-biphenyl-4-yl-ureido)-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Methanesulfonyl-2-(3-cyclohexyl-ureido)-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Methanesulfonyl-2-(3-ethyl-thioureido)-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-(3-isopropyl-thioureido)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanoethyl-amide, 3-Methanesulfonyl-2-(3-phenyl-thioureido)-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-(thiophene-2-sulfonylamino)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-Methanesulfonyl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide, 3-Methanesulfonyl-2-benzenesulfonylamino-propionicacid cyanoethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-amide,4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,3-Methanesulfonyl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanoethyl-amide,3-Methanesulfonyl-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-2-nitro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-acrylamide,3-Methanesulfonyl-2,2-dimethyl-propionic acid cyanoethyl-amide,3-Methanesulfonyl-2-(2-methoxy-acetylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-phthalamic acid,N-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-succinamic acid,3-[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethylcarbamoyl]-acrylicacid, [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidisobutyl ester,[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanomethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid hexylester, [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acid methylester, [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamic acidethyl ester, [1-(Cyanoethyl-carbamoyl)-2-methanesulfonyl-ethyl]-carbamicacid 9H-fluoren-9-ylmethylester,3-Naphthalen-2-yl-2-acetylamino-propionic acid cyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Naphthalen-2-yl-2-(3-benzyl-ureido)-propionic acidcyanomethyl-amide, 3-Naphthalen-2-yl-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Naphthalen-2-yl-2-(3-cyclohexyl-ureido)-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Naphthalen-2-yl-2-(3-ethyl-thioureido)-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-(thiophene-2-sulfonylamino)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide, 3-Naphthalen-2-yl-2-benzenesulfonylamino-propionicacid cyanomethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,4-Acetylamino-N-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,3-Naphthalen-2-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-nitro-benzamide,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-acrylamide,3-Naphthalen-2-yl-2,2-dimethyl-propionic acid cyanomethyl-amide,3-Naphthalen-2-yl-2-(2-methoxy-acetylamino)-propionic acidcyanomethyl-amide,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic acid,N-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-succinamic acid,3-[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethylcarbamoyl]-acrylicacid, [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidisobutyl ester,[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidhexyl ester,[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid methylester, [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidethyl ester,[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid9H-fluoren-9-ylmethyl ester, 3-Naphthalen-2-yl-2-acetylamino-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Naphthalen-2-yl-2-(3-benzyl-ureido)-propionic acidcyanoethyl-amide, 3-Naphthalen-2-yl-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanoethyl-amide, 3-Naphthalen-2-yl-2-(3-biphenyl-4-yl-ureido)-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Naphthalen-2-yl-2-(3-cyclohexyl-ureido)-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Naphthalen-2-yl-2-(3-ethyl-thioureido)-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-(3-isopropyl-thioureido)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanoethyl-amide, 3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-(thiophene-2-sulfonylamino)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-Naphthalen-2-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(4-methoxy-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide, 3-Naphthalen-2-yl-2-benzenesulfonylamino-propionicacid cyanoethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,2-Propyl-pentanoic acid[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,Thiophene-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide,4-Acetylamino-N-[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,3-Naphthalen-2-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanoethyl-amide,3-Naphthalen-2-yl-2-(3-1H-indol-3-yl-propionylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,3-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,4-Chloromethyl-N-[1-(cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-fluoro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-2-nitro-benzamide,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-acrylamide,3-Naphthalen-2-yl-2,2-dimethyl-propionic acid cyanoethyl-amide,3-Naphthalen-2-yl-2-(2-methoxy-acetylamino)-propionic acidcyanoethyl-amide,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-oxalamic acidmethyl ester,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-phthalamic acid,N-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-succinamic acid,3-[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethylcarbamoyl]-acrylicacid, [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidisobutyl ester,[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid butylester, [1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidcyanomethyl ester,[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidbut-3-enyl ester,[1-(Cyanomethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid hexylester, [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidtert-butyl ester,[1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acid methylester, [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamic acidethyl ester, [1-(Cyanoethyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamicacid 9H-fluoren-9-ylmethylester,3-Benzo[b]thiophen-3-yl-2-acetylamino-propionic acid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanomethyl-amide, 3-Benzo[b]thiophen-3-yl-2-(3-benzyl-ureido)-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-o-tolyl-ureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-cyclohexyl-ureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(thiophene-2-sulfonylamino)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-methoxy-benzenesulfonylamino)-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(quinoline-6-sulfonylamino)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-benzenesulfonylamino-propionic acidcyanomethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,2-Propyl-pentanoic acid[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,Thiophene-2-carboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-amide,4-Acetylamino-N-[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,3-Benzo[b]thiophen-3-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-1H-indol-3-yl-propionylamino)-propionicacid cyanomethyl-amide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-acrylamide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-acrylamide,3-Benzo[b]thiophen-3-yl-2,2-dimethyl-propionic acid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(2-methoxy-acetylamino)-propionic acidcyanomethyl-amide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-oxalamicacid methyl ester,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-phthalamicacid,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-succinamicacid,3-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethylcarbamoyl]-acrylicacid, [2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamicacid isobutyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acidbutyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acidcyanomethyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acidbut-3-enyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acidhexyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acidtert-butyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acidmethyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acidethyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-carbamic acid9H-fluoren-9-ylmethyl ester,3-Benzo[b]thiophen-3-yl-2-acetylamino-propionic acid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethylsulfanyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-cyano-phenyl)-ureido]-propionic acidcyanoethyl-amide, 3-Benzo[b]thiophen-3-yl-2-(3-benzyl-ureido)-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-o-tolyl-ureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(S)-(1-phenyl-ethyl)-ureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(2,6-dimethyl-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(3-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(1,1,3,3-tetramethyl-butyl)-ureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-indan-5-yl-ureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(2-phenyl-cyclopropyl)-ureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-adamantan-1-yl-ureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-biphenyl-4-yl-ureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-phenoxy-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-ureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-cyclohexyl-ureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-benzo[1,3]dioxol-5-yl-ureido)-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(2-fluoro-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-methyl-benzyl)-ureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-phenethyl-ureido)-ureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(3,4,5-trimethoxy-phenyl)-ureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-ethyl-thioureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-isopropyl-thioureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-phenyl-thioureido)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(7,7-dimethyl-2-oxo-bicyclo[2.2.1]hept-1-ylmethanesulfonylamino)-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(thiophene-2-sulfonylamino)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-trifluoromethoxy-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-tert-butyl-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-chloro-benzenesulfonylamino)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(4-methoxy-benzenesulfonylamino)-propionicacid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(quinoline-6-sulfonylamino)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-benzenesulfonylamino-propionic acidcyanoethyl-amide, 1-Methyl-1H-indole-2-carboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,2-Propyl-pentanoic acid[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,1-Methyl-cyclopropanecarboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,Thiophene-2-carboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-3-trifluoromethyl-benzamide,Biphenyl-2-carboxylic acid[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-amide,4-Acetylamino-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide,3-Benzo[b]thiophen-3-yl-2-(2-1H-indol-3-yl-acetylamino)-propionic acidcyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-1H-indol-3-yl-propionylamino)-propionicacid cyanoethyl-amide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-4-(1H-indol-3-yl)-butyramide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide,3-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,4-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-benzamide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-2-fluoro-benzamide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanomethyl-carbamoyl)-ethyl]-2-nitro-benzamide,3-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide,4-Chloromethyl-N-[2-benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-benzamide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-2-fluoro-benzamide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-2-nitro-benzamide,3-Benzo[b]thiophen-3-yl-2,2-dimethyl-propionic acid cyanoethyl-amide,3-Benzo[b]thiophen-3-yl-2-(2-methoxy-acetylamino)-propionic acidcyanoethyl-amide,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-oxalamic acidmethyl ester,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-phthalamicacid,N-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-succinamicacid,3-[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethylcarbamoyl]-acrylicacid, [2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamicacid isobutyl ester, 1-Cyanomethyl-pyrrolidine-2-carboxylic acidcarbamoylmethyl-amide 1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-2-methyl-propyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-2-hydroxy-ethyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-4-guanidino-butyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-2-phenyl-ethyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid[1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid[1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide3-[(1-Cyanomethyl-pyrrolidine-2-carbonyl)-amino]-succinamic acidD-1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-3-methyl-butyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-cyclohexyl)-amide 1-Cyanomethyl-pyrrolidine-2-carboxylicacid [1-carbamoyl-2-(4-trifluoromethyl-benzylsulfanyl)-ethyl]-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid[1-carbamoyl-2-(4-fluoro-benzylsulfanyl)-ethyl]-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid[1-carbamoyl-2-(4-fluoro-phenylmethanesulfonyl)-ethyl]-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid (3-carbamoyl-phenyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid[1-carbamoyl-2-(1-methyl-1H-imidazol-4-yl)-ethyl]-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-2-pyridin-4-yl-ethyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-3-methyl-butyl)-amide1-Cyanomethyl-pyrrolidine-2-carboxylic acid methyl ester1-Cyanomethyl-pyrrolidine-2-carboxylic acidN-(2-Cyanoethyl)-4-(4-dimethylamino-phenylazo)-benzenesulfonamideN-(2-Cyanoethyl)-4-trifluoromethoxy-benzenesulfonamide4-tert-Butyl-N-(2-cyanoethyl)-benzenesulfonamide4-Bromo-N-(2-cyanoethyl)-benzenesulfonamide4-Chloro-N-(2-cyanoethyl)-benzenesulfonamideN-(2-Cyanoethyl)-4-methoxy-benzenesulfonamideN-[4-(2-Cyanoethyl-sulfamoyl)-phenyl]-acetamideN-(2-Cyanoethyl)-4-methyl-benzenesulfonamideN-(2-Cyanoethyl)-benzenesulfonamideN-(2-Cyanoethyl)-C-phenyl-methanesulfonamideC,C,C-Trichloro-N-(2-cyanoethyl)-methanesulfonamide Butane-1-sulfonicacid (2-cyanoethyl)-amide Naphthalene-1-sulfonic acid(2-cyanoethyl)-amide Octane-1-sulfonic acid (2-cyanoethyl)-amideN-(2-Cyanoethyl)-2,4,6-triisopropyl-benzenesulfonamideN-(2-Cyanoethyl)-2-trifluoromethyl-benzenesulfonamideN-[5-(2-Cyanoethyl-sulfamoyl)-4-methyl-thiazol-2-yl]-acetamide2-Bromo-N-(2-cyanoethyl)-benzenesulfonamideN-(2-Cyanoethyl)-2,4,6-trimethyl-benzenesulfonamide Thiophene-2-sulfonicacid (2-cyanoethyl)-amide N-(2-Cyanoethyl)-3-nitro-benzenesulfonamide1-(2-Cyanoethyl)-3-(4-nitro-phenyl)-thiourea 1-(2-Cyano1-(2-Cyano-ethyl)-3-phenyl-thioureaethyl)-3-phenyl-thiourea1-(2-Cyanoethyl)-3-(4-trifluoromethoxy-phenyl)-thiourea1-(2-Cyanoethyl)-3-(4-methylsulfanyl-phenyl)-thiourea1-(2-Cyanoethyl)-3-(3,4,5-trimethoxy-phenyl)-thiourea1-(2-Cyanoethyl)-3-naphthalen-1-yl-thiourea1-Benzyl-3-(2-cyanoethyl)-thiourea 1-Acetyl-3-(2-cyanoethyl)-thiourea1-(4-Azido-phenyl)-3-(2-cyanoethyl)-thiourea1-(2-Cyanoethyl)-3-(3-cyano-phenyl)-thiourea1-(2-Cyano1-(2-Cyano-ethyl)-3-(4-ethyl-phenyl)-thioureaethyl)-3-(4-ethyl-phenyl)-thiourea1-(2-Cyano1-(2-Cyano-ethyl)-3-(4-cyano-phenyl)-thioureaethyl)-3-(4-cyano-phenyl)-thiourea1-Carbamoylmethyl-pyrrolidine-2-carboxylic acid(1-carbamoyl-3-methyl-butyl)-amide1-(2-Cyanoethyl)-3-pyridin-4-yl-thiourea1-(2-Cyanoethyl)-3-(2,3,4-trifluoro-phenyl)-thiourea1-(2-Cyanoethyl)-3-(2,6-difluoro-phenyl)-thiourea1-(4-Bromo-phenyl)-3-(2-cyanoethyl)-thiourea1-(2-Cyanoethyl)-3-(4-methoxy-phenyl)-thiourea1-(2-Cyanoethyl)-3-m-tolyl-thiourea 1-(2-Cyanoethyl)-3-p-tolyl-thiourea1-(2-Cyanoethyl)-3-cyclohexyl-urea 1-(2-Cyanoethyl)-3-o-tolyl-urea1-(2-Cyanoethyl)-3-(2-methoxy-phenyl)-urea[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acidbutyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acidcyanomethyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acidbut-3-enyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acid2-isopropyl-5-methyl-cyclohexyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acidhexyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acidtert-butyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acidmethyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acidethyl ester,[2-Benzo[b]thiophen-3-yl-1-(cyanoethyl-carbamoyl)-ethyl]-carbamic acid9H-fluoren-9-ylmethylester, or a pharmaceutically acceptable salt orprodrug thereof.
 34. A pharmaceutical composition comprising a compoundaccording to claim 1 and a pharmaceutically acceptable carrier, diluentand/or excipient.
 35. The pharmaceutical composition according to claim34 comprising a further pharmaceutically active compound.
 36. Thepharmaceutical composition according to claim 34, wherein the compoundis present as a pharmaceutically acceptable salt or a pharmaceuticallyactive solvate.
 37. The pharmaceutically active composition according toclaim 34, wherein the pharmaceutically active compound is either aloneor in combination with any of the ingredients of the composition presentin a multitude of individualized dosages and/or administration forms.38. Use of a compound according to claim 1 for the manufacture of amedicament for the treatment and/or prevention of a disease, wherebypreferably the disease involves an abnormal cell proliferation, anundesired cell proliferation, an abnormal mitosis and/or an undesiredmitosis, whereby the compound is a compound according to any of claims 1to 33 claim 1 or a pharmaceutically acceptable salt or a prodrugthereof.
 39. The use according to claim 38, wherein the compound isacting on an enzymatic activity involved in the regulation of celldivision and/or cell cycle or part thereof, preferably the part of thecell cycle is mitosis.
 40. The use according to claim 38, wherein thedisease is selected from the group comprising neurodegenerativediseases, stroke, inflammatory diseases, immune based disorders,infectious diseases, heart diseases, cardiovascular diseases and cellproliferative diseases.
 41. The use according to claim 40, wherein theneurodegenerative disease is selected from the group comprisingAlzheimer's disease, Huntington's disease, Parkinson's disease,peripheral neuropathy, progressive supranuclear palsy, corticobasaldegeneration, frontotemporal dementia, synucleinopathies, multiplesystem atrophy, amyotrophic lateral sclerosis, prion diseases and motorneuron diseases.
 42. The use according to claim 40, wherein theinfectious disease is selected from the group comprising fungal, viral,bacterial and parasite infection.
 43. The use according to claim 42,wherein the fungal infection is selected from the group comprisinggynaecological and dermatological infection.
 44. The use according toclaim 42, wherein the fungal infection is caused by Histoplasma,Coccidioides, Cryptococcus, Blastomyces, Paracoccidioides, Aspergillus,Sporothrix, Rhizopus, Absidia, Mucor, Hormodendrum, PhialophoraMicrosporum, Epidermophyton, Rhinosporidum or by a yeast, preferablyCandida or Cryptococcus.
 45. The use according to claim 42, wherein thefungal infection causes a disorder selected from the group comprisingringworm, candidiasis, coccidioidomycosis, blastomycosis, aspergillosis,cryptococcosis, histioplasmosis, paracoccidiomycosis, zygomycosis,sporotrichiosis, mycotic keratitis, nail hair and skin disease,lobomycosis, chromoblastomycosis and mycetoma.
 46. The use according toclaim 42, wherein the bacterial infection is selected from the groupcomprising infections caused by Gram-positive and by Gram-negativebacteria.
 47. The use according to claim 46, wherein the bacterialinfection is caused by Staphylococcus, Clostridium, Streptococcus,Listeria, Salmonella, Bacillus, Escherichia, Mycobacteria, Serratia,Enterobacter, Enterococcus, Nocardia, Hemophilus, Neisseria, Proteus,Yersinia, Helicobacter or Legionella.
 48. The use according to claim 42,wherein the bacterial infection causes a disorder selected from thegroup comprising pneumonia, diarrhea, dysentery, anthrax, rheumaticfever, toxic shock syndrome, mastoiditis, meningitis, gonorrhea, typhoidfever, brucellis, Lyme disease, gastroenteritis, tuberculosis, cholera,tetanus and bubonic plague.
 49. The use according to claim 42, whereinthe viral infection is selected from the group comprising infectionscaused by retrovirus (HIV), Papilloma virus, Polio virus, Epstein-Barr,Herpes virus, Hepatitis virus, Papova virus, Influenza virus, Rabies,JC, encephalitis causing virus or hemorrhagic fever causing virus. 50.The use according to claim 42, wherein the parasite infection isselected from the group comprising infections caused by Trypanosoma,Leishmania, Trichinella, Echinococcus, Nematodes, Classes CestodaTrematoda, Monogenea, Toxoplasma, Giardia, Balantidium, Paramecium,Plasmodium, or Entamoeba.
 51. The use according to claim 40, wherein thecell proliferative disorder is selected from the group comprisingneoplastic and non-neoplastic disorders.
 52. The use according to claim51, wherein the neoplastic cell proliferative disorder is selected fromthe group comprising solid tumor, lymphoma and leukemia.
 53. The useaccording to claim 52, wherein the solid tumor is selected from thegroup comprising carcinoma, sarcoma, osteoma, fibrosarcoma, andchondrosarcoma.
 54. The use according to claim 51, wherein theneoplastic cell proliferative disorder is selected from the groupcomprising breast cancer, prostate cancer, colon cancer, brain cancer,lung cancer, pancreatic cancer, gastric cancer, bladder cancer andkidney cancer.
 55. The use according to claim 51, wherein thenon-neoplastic cell proliferative disorder is a fibrotic disorder,preferably the fibrotic disorder is fibrosis.
 56. The use according toclaim 51, wherein the non-neoplastic cell proliferative disorder isselected from the group comprising prostatic hypertrophy, endometriosis,psoriasis, tissue repair and wound healing.
 57. The use according toclaim 40, wherein the immune based/inflammatory disease is an autoimmunedisease or disorder.
 58. The use according to claim 40, wherein theimmune based/inflammatory disease is selected from the group comprisingrheumatoid arthritis, glomerulonephritis, systemic lupus erythematosusassociated glomerulonephritis, irritable bowel syndrome, bronchialasthma, multiple sclerosis, pemphigus, pemphigoid, scleroderma,myasthenia gravis, autoimmune haemolytic and thrombocytopenic states,Goodpasture's syndrome, pulmonary hemorrhage, vasculitis, Crohn'sdisease and dermatomyositis.
 59. The use according to claim 40, whereinthe immune based and/or inflammatory disease is an inflammatorycondition.
 60. The use according to claim 40, wherein the immune basedand/or inflammatory disease is selected from the group comprisinginflammation associated with burns, lung injury, myocardial infarction,coronary thrombosis, vascular occlusion, post-surgical vascularreocclusion, artherosclerosis, traumatic central nervous system injury,ischemic heart disease and ischemia-reperfusion injury, acuterespiratory distress syndrome, systemic inflammatory response syndrome,multiple organ dysfunction syndrome, tissue graft rejection andhyperacute rejection of transplanted organs.
 61. Use of a compound as apharmaceutical in drug potentiation applications, whereby the compoundis a compound as described in claim 1, or a pharmaceutically acceptablesalt or a prodrug thereof.
 62. The use according to claim 61, wherebythe drug potentiation application is the manufacture of a medicament foruse in drug potentiation applications, wherein the medicament is for thetreatment of a diseases which involves an abnormal cell proliferation,an undesired cell proliferation, an abnormal mitosis and/or an undesiredmitosis.
 63. The use according to claim 1, wherein the medicamentcomprises the compound or a pharmaceutically acceptable salt or prodrugthereof in a therapeutically effective amount together with apharmaceutically acceptable carrier and/or diluent and/or adjuvant. 64.The use according to claim 1, wherein the medicament for theadministration to a patient is selected from the group comprisinghumans, canine, bovine, feline, porcine, caprine, equine, ovine animals,domesticated animals, reptiles, birds, lagomorphs, rodents, amphibians,fish, arthropods, valuable non-domesticated animals, and zoo animals.65. The use according to claim 1 wherein the medicament is for theadministration to a mammal, preferably to a human being.
 66. The useaccording to claim 1 wherein the medicament is for administration via anadministration route which is selected from the groups injection,infusion, suppository, tablet, transdermal patch, aerosol, oradministered orally, subcutaneously, intravenously, intranasally,transdermally, intraperitoneally, intramuscularly, intrapulmonary,vaginally, rectally, via an implanted reservoir, or intraocularly. 67.Use of a compound according to claim 1 as inhibitor to a rotamase. 68.Use of a compound for the manufacture of a kit for the inhibition of arotamase and/or for quantification of the amount of rotamase in asample, whereby the compound is a compound as described in any of thepreceding claims, a pharmaceutically acceptable salt and/or a prodrugthereof, whereby the kit preferably comprises a standardized amount ofor solution of said compound or a pharmaceutically acceptable salt orprodrug thereof.
 69. Use of a compound for removing a rotamase from asample or for identifying a rotamase in a sample, whereby the compoundis a compound as described in claim 1, or a pharmaceutically acceptablesalt or a prodrug thereof.
 70. Use of a compound for the manufacture ofor in an affinity device, whereby the compound is a compound asdescribed in claim 1, or a pharmaceutically acceptable salt or a prodrugthereof, whereby preferably the affinity device is a chromatographiccolumn.
 71. The use according to claim 70, whereby the compound is boundto a chromatographic support.
 72. The use according to claim 70, wherebythe device is for removal and/or identifying of a rotamase from/in asample.
 73. Use according to claim 69, wherein the sample is abiological sample, preferably a sample which is selected from the groupcomprising blood, lymph, saliva, tissue samples and bacterial, fungal,plant, viral and mammalian cell cultures.
 74. Use of a derivative or ofa precursor of a compound of formula (I) according to claim 1, whichupon chemical transformation is converted into another compound offormula (I), as inhibitor of or to a rotamase and/or the manufacture ofa medicament.
 75. The use according to claim 74, whereby the chemicaltransformation is selected from the group comprising hydrolysis,oxidation and reduction, whereby such transformation is preferablycarried out in vivo or in vitro.
 76. The use according to claim 38,whereby the compound or a pharmaceutically acceptable salt or prodrugthereof is chiral.
 77. The use according to claim 76, whereby thecompound or a pharmaceutically acceptable salt or prodrug thereof, hasat least one amino acid side chain, whereby the amino acid side chain isin the (S) or L-configuration or in the (R) or D-configuration.
 78. Theuse according to claim 39, wherein the enzyme, preferably a rotamase,regulates a part of the cell cycle, preferably the part of the cellcycle is mitosis.
 79. The use according to claim 38, wherein therotamase is a mammalian rotamase, preferably a human rotamase, morepreferably hPin1.
 80. The use according to claim 38, whereby thecompound or a pharmaceutically acceptable salt or prodrug thereofcomprises a label.
 81. The use according to claim 80, whereby thecompound or a pharmaceutically acceptable salt or prodrug thereofcomprises at least one label, whereby the label is selected from thegroup comprising radioactive isotopes, heavy isotopes, immune labels,coloured labels and fluorescent labels.
 82. The use according to claim80, whereby the compound or a pharmaceutically acceptable salt orprodrug thereof, comprises at least one label, whereby the label isselected from the group comprising ¹⁴C, ¹³C, ¹⁵N, and ³H.
 83. The useaccording to claim 80, whereby the compound or a pharmaceuticallyacceptable salt or prodrug thereof, comprises at least one immune label,whereby the label is selected from the group comprising antibodies andantigens.
 84. The use according to claim 80, whereby the compound or apharmaceutically acceptable salt or prodrug thereof, comprises at leastone colored and/or fluorescent label, whereby the fluorescent label isselected from the group comprising fluorescein, 6-FAM, HEX, TET, CY-5,CY-3, CY-7, Texas Red.
 85. A method of treating a patient suffering froma disease which involves an abnormal cell proliferation, an undesiredcell proliferation, an abnormal mitosis and/or an undesired mitosis byadministering a compound of claim
 1. 86. A method of treating a patientfor drug potentiation by administering a pharmaceutical formulation ormedicaments according to claim
 1. 87. A compound as described in claim1, which is selected from the group comprising3-(1H-Indol-3-yl)-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-(1H-Indol-3-yl)-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-(1H-Indol-3-yl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-(4-Hydroxy-phenyl)-2-(3-ethyl-thioureido)-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-(4-Hydroxy-phenyl)-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide 3-Phenyl-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide, 3-Phenyl-2-[3-(4-nitro-phenyl)-thioureido]-propionicacid cyanomethyl-amide, 3-Phenyl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide,3-Phenyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Phenyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Phenyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide 3-Methylsulfanyl-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-isopropyl-thioureido)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-Methylsulfanyl-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Methylsulfanyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide 3-Methanesulfonyl-2-(3-ethyl-thioureido)-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-Methanesulfonyl-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Methanesulfonyl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide 3-Naphthalen-2-yl-2-(3-ethyl-thioureido)-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide, 3-Naphthalen-2-yl-2-(3-phenyl-thioureido)-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Naphthalen-2-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionic acidcyanomethyl-amide3-Benzo[b]thiophen-3-yl-2-(3-ethyl-thioureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-isopropyl-thioureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-nitro-phenyl)-thioureido]-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-(3-phenyl-thioureido)-propionic acidcyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-trifluoromethoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-{3-[4-(2,2,2-trifluoro-ethyl)-phenyl]-thioureido}-propionicacid cyanomethyl-amide,3-Benzo[b]thiophen-3-yl-2-[3-(4-methoxy-phenyl)-thioureido]-propionicacid cyanomethyl-amide, or a pharmaceutically acceptable salt or aprodrug thereof.